|
Displacement of [1251][Sar1,IIe8]AII from rabbit aorta Angiotensin II receptor, type 1
|
Oryctolagus cuniculus
|
54.0
nM
|
|
|
Inhibitory activity against Angiotensin II receptor, type 1 induced contractions in isolated rabbit aortic rings
|
Oryctolagus cuniculus
|
3.0
nM
|
|
|
Compound was evaluated for in vitro potency against angiotensin II receptor, type 1 in isolated rabbit aorta; value ranges from 8.27-8.70
|
Oryctolagus cuniculus
|
5.37
nM
|
|
|
Potency to antagonize the ability of angiotensin II to contract rabbit aorta
|
Oryctolagus cuniculus
|
3.715
nM
|
|
|
pA2 value determined in vitro against angiotensin II receptor, type 1 using rabbit aortic rings
|
Oryctolagus cuniculus
|
3.715
nM
|
|
|
Binding affinity against angiotensin II receptor type 1 (AT1) from rat liver.
|
None
|
5.0
nM
|
|
|
Binding affinity for Angiotensin II receptor, type 1 measured by ability to displace [125I]- A II from its specific binding site in rat liver membrane
|
None
|
14.0
nM
|
|
|
Concentration required to inhibit binding of radioligand [125I]AII to angiotensin II receptor, type 1 in rat adrenal glomerulosa tissue
|
None
|
19.0
nM
|
|
|
Binding affinity for rat angiotensin II receptor, type 1
|
None
|
6.7
nM
|
|
|
Inhibition of specific binding of [125I]angiotensin-II to angiotensin 1 receptor in rat lung membrane preparation
|
None
|
35.0
nM
|
|
|
In vitro antagonistic activity by displacement of [125I]-Sar1-Ile8-A II at the rat adrenal cortical aorta Angiotensin II receptor, type 1
|
None
|
19.0
nM
|
|
|
Inhibition of [125I]angiotensin-II binding to the angiotensin II receptor type 1 in rat uterine membranes
|
None
|
36.0
nM
|
|
|
Inhibitory concentration that gives 50% displacement of specific binding at labeled angiotensin II type 1 receptor in rat adrenal cortical membranes.
|
None
|
19.0
nM
|
|
|
Inhibitory concentration was evaluated by measuring displacement of [3H]AII from rat liver Angiotensin II receptor, type 1
|
Rattus norvegicus
|
59.0
nM
|
|
|
Compound was evaluated for binding affinity against angiotensin II receptor, type 1 in rat liver
|
None
|
14.63
nM
|
|
|
In vitro inhibitory activity against rat Angiotensin II receptor, type 1 expressed in CHO cells
|
None
|
40.0
nM
|
|
|
Concentration required for 50% inhibition of binding against Angiotensin II receptor, type 1 in rat adrenal cortex
|
None
|
8.2
nM
|
|
|
In vitro binding affinity for rat liver angiotensin II receptor type 1, determined by displacement of the specially bound [3H]AII radioligand
|
None
|
59.0
nM
|
|
|
Inhibitory activity against Angiotensin II receptor type 1 in rat adrenal membrane
|
Rattus norvegicus
|
19.0
nM
|
|
|
Inhibitory activity against Angiotensin II receptor, type 1 in rat vascular smooth muscle
|
None
|
20.0
nM
|
|
|
Inhibitory concentration against binding of [125I]angiotensin II to rat liver expressing Angiotensin II receptor
|
None
|
5.0
nM
|
|
|
Inhibitory concentration against [125 I]Ang II binding to rat pituitary membranes Angiotensin II receptor type 1 without 0.2% bovine serum albumin
|
Rattus norvegicus
|
1.8
nM
|
|
|
Tested for inhibitory concentration against AT1 receptor binding affinity in rat liver
|
None
|
5.0
nM
|
|
|
Displacement of [3H]angiotensin II from Angiotensin II type 1 receptor in rat adrenal cortical membrane
|
None
|
11.0
nM
|
|
|
In vivo percent inhibition of Angiotensin II receptor, type 1 induced increase in diastolic blood pressure in pithed rat at 3 mg/kg i.d.
|
None
|
74.0
nM
|
|
|
Tested for inhibition of Angiotensin II receptor, type 1 in the absence of bovine serum albumin (BSA)
|
None
|
8.0
nM
|
|
|
In vitro inhibition of specific binding of [125 I] A II to rat liver membrane.
|
None
|
34.7
nM
|
|
|
Binding affinity against angiotensin II receptor from rat liver; n=8
|
None
|
14.6
nM
|
|
|
Inhibition of [125I]AII binding to angiotensin II receptor of bovine adrenal cortex
|
Bos taurus
|
350.0
nM
|
|
|
Ability to displace [125I]- labelled [Sar1,Ileu8] from angiotensin II receptor of bovine adrenal cortex membranes
|
None
|
420.0
nM
|
|
|
Binding affinity expressed as inhibitory concentration towards bovine adrenal cortex angiotensin II receptor was measured
|
None
|
330.0
nM
|
|
|
Displacement of [125 I]-AII (0.2 nM) from bovine adrenal cortical membrane angiotensin II (AII) receptor at 10e-7 M
|
Bos taurus
|
150.0
nM
|
|
|
Inhibition of [125l]-All binding to bovine adrenal cortex
|
Bos taurus
|
120.0
nM
|
|
|
Binding affinity for angiotensin II receptor of bovine adrenal cortex
|
Bos taurus
|
300.0
nM
|
|
|
In vitro binding affinity to angiotensin II receptor in bovine adrenal cortex
|
None
|
330.0
nM
|
|
|
In vitro Angiotensin II receptor antagonism in bovine adrenal cortex tissue.
|
None
|
330.0
nM
|
|
|
Inhibition of specific binding of [125I]angiotensin II (0.2 nM) to angiotensin II receptor in bovine adrenal cortex
|
Bos taurus
|
150.0
nM
|
|
|
Displacement of monoiodinated angiotensin II from guinea-pig adrenal gland angiotensin II receptor
|
Cavia porcellus
|
18.0
nM
|
|
|
Inhibition of [125I]AII binding to guinea pig adrenal membrane
|
Cavia porcellus
|
8.0
nM
|
|
|
In vitro binding affinity against Angiotensin II receptor in rabbit aorta rings
|
Oryctolagus cuniculus
|
1.585
nM
|
|
|
Binding affinity towards Angiotensin receptor from rabbit aorta
|
Oryctolagus cuniculus
|
50.0
nM
|
|
|
Binding against Angiotensin II receptor in a radioligand binding assay using [125I]-Sar1-Ile8 angiotensin-II as radioligand in rat adrenal cortical membranes
|
Rattus norvegicus
|
5.7
nM
|
|
|
Binding affinity expressed as inhibitory concentration against angiotensin II of rat adrenal cortex
|
None
|
57.0
nM
|
|
|
Displacement of [3H]-AII from the Angiotensin II receptor isolated from the liver of rats
|
Rattus norvegicus
|
4.6
nM
|
|
|
Concentration required for 50% inhibition of binding against Angiotensin II receptor in the rat adrenal cortex tissue
|
None
|
82.0
nM
|
|
|
In vitro Angiotensin II receptor antagonist activity in rat adrenal cortex tissue.
|
None
|
82.0
nM
|
|
|
Tested for in vitro binding affinity against angiotensin II receptor of rat liver
|
None
|
31.62
nM
|
|
|
Competitive inhibition of Angiotensin II receptor binding of radiolabeled AII to rat adrenal glomerulosa tissue by 50%
|
None
|
13.0
nM
|
|
|
Inhibition of specific binding of [3H]angiotensin II (2 nM) to rat adrenal cortical microsomes
|
None
|
19.0
nM
|
|
|
Inhibition of specific binding of [3H]angiotensin II (AII) in rat adrenal cortical membranes
|
None
|
26.0
nM
|
|
|
Tested in vitro for inhibition of [125I]AII to rat uterine membranes
|
None
|
36.0
nM
|
|
|
Binding affinity against angiotensin II receptor in rat smooth muscle cell preparations
|
Rattus norvegicus
|
26.0
nM
|
|
|
Inhibition of radioligand [3H]angiotensin II binding to angiotensin II receptor of rat adrenal cortical membrane
|
None
|
19.0
nM
|
|
|
Tested for binding affinity against angiotensin II receptor in bovine adrenal cortex
|
None
|
160.0
nM
|
|
|
In vitro inhibitory activity against angiotensin II rabbit aorta AT1 receptor using radioligand [125I]-Sar Ile-AII
|
Oryctolagus cuniculus
|
40.0
nM
|
|
|
In vitro binding affinity for angiotensin II AT1 receptor in rabbit aorta
|
Oryctolagus cuniculus
|
50.0
nM
|
|
|
Tested for binding affinity against angiotensin II receptor in rat adrenal cortex
|
None
|
8.2
nM
|
|
|
Displacement of [125I]-Sar1-Ile8-A II from rat adrenal Angiotensin-1 (AT-1) receptor
|
None
|
3.6
nM
|
|
|
In vitro for inhibition of [125I]-angiotensin II (0.1 nM) binding to angiotensin II receptor type 1 in membrane fractions of bovine adrenal cortex
|
None
|
120.0
nM
|
|
|
Concentration that gives 50% inhibition for binding of 125-I-[Sar1, IIe8] angiotensin to Angiotensin II receptor, type 1 in bovine adrenal cortex membrane.
|
None
|
425.0
nM
|
|
|
Inhibition of [125I]angiotensin binding to a guinea pig adrenal membrane preparation which corresponds to Angiotensin II receptor, type 1
|
Cavia porcellus
|
18.0
nM
|
|
|
Compound was tested for in vitro inhibition of specific binding of [I-125]AII to Angiotensin II receptor, type 1 in guinea pig adrenal membrane preparation
|
Cavia porcellus
|
18.0
nM
|
|
|
In vitro inhibitory activity against angiotensin II receptor type 1, in human adrenal membrane preparations.
|
None
|
88.0
nM
|
|
|
Inhibition against human angiotensin II receptor, type 1 (AG2-R)
|
None
|
28.0
nM
|
|
|
Inhibitory activity against angiotensin I converting enzyme (ACE)
|
None
|
19.0
nM
|
|
|
Evaluation of Angiotensin II antagonistic activity by displacement of [125I]-Sar Ile-AII at the rabbit aorta Angiotensin II receptor, type 1
|
Oryctolagus cuniculus
|
40.0
nM
|
|
|
In vitro antagonist activity against angiotensin II receptor type 1 in rabbit aorta using [125I]-Sar, Ile AII.
|
Oryctolagus cuniculus
|
54.0
nM
|
|
|
In vitro antagonist activity against angiotensin II receptor type 1 in rabbit aorta using [125I]-Sar, Ile AII.
|
Oryctolagus cuniculus
|
54.0
nM
|
|
|
Displacement of [125I]-Sar1-Ile8-A II at the rabbit aorta angiotensin II receptor, type 1
|
Oryctolagus cuniculus
|
50.0
nM
|
|
|
In vitro antagonistic activity for AT1 receptor by displacing 125I[Sar, ILe8]AII radioligand in rabbit aorta membrane using 0.2% bovine serum albumin (BSA)
|
Oryctolagus cuniculus
|
19.0
nM
|
|
|
In vitro antagonistic activity for angiotensin II receptor, type 1 by displacing 125I[Sar, ILe8 ]AII radioligand in rabbit aorta membrane without using bovine serum albumin (BSA)
|
Oryctolagus cuniculus
|
50.0
nM
|
|
|
In vitro inhibitory activity against Angiotensin II receptor, type 1 in rabbit aorta membrane preparations.
|
Oryctolagus cuniculus
|
30.0
nM
|
|
|
In vivo inhibitory activity against pressor response induced by exogenously administered angiotensin-II (0.1 ug/kg, i.v.) in dog at dose 3 mg/kg after intravenous administration
|
Canis lupus familiaris
|
76.0
%
|
|
|
Inhibitory activity against Ang II-induced proliferation of human aortic smooth muscle cells in a dose dependent manner
|
Homo sapiens
|
0.71
nM
|
|
|
The compound was evaluated for the percentage of inhibition of A II pressor response in rhesus monkey for peroral administration.
|
Cercopithecidae
|
10.32
%
|
|
|
The compound was evaluated for the percentage of inhibition of A II pressor response in rhesus monkeys for intravenous administration
|
Cercopithecidae
|
0.32
%
|
|
|
Inhibition of AII pressor response by the compound in conscious, normotensive monkey, at 0.3 (mg/kg) intravenous dose
|
Cercopithecidae
|
49.0
%
|
|
|
Inhibition of AII pressor response by the compound in conscious, normotensive monkey, at 10 (mg/kg) peroral dose
|
Cercopithecidae
|
50.0
%
|
|
|
Tested for inhibition of Angiotensin II-induced pressor response in rabbit aorta
|
Oryctolagus cuniculus
|
24.0
nM
|
|
|
Inhibitory concentration against [125I]angiotensin II(AII) induced contraction in rabbit aorta by 50%
|
Oryctolagus cuniculus
|
89.0
nM
|
|
|
Antagonism of angiotensin-II mediated contraction of rabbit aortic rings expressed as pA2 (in vitro)
|
Oryctolagus cuniculus
|
7.943
nM
|
|
|
Antagonism against A-2 induced contraction of aortic rings from rabbit.
|
Oryctolagus cuniculus
|
2.951
nM
|
|
|
Evaluated for antagonism of AII contracted rabbit aortic rings
|
Oryctolagus cuniculus
|
7.943
nM
|
|
|
Inhibition of angiotensin II induced contraction in thoracic aortic rings from New Zealand rabbits
|
Oryctolagus cuniculus
|
1.585
nM
|
|
|
Potency of the Angiotensin II-induced contraction of rabbit aortic strips
|
Oryctolagus cuniculus
|
2.512
nM
|
|
|
Tested for inhibitory activity against angiotensin II induced contraction in rabbit aortic rings
|
Oryctolagus cuniculus
|
1.585
nM
|
|
|
Inhibition of angiotensin II-induced contractions in rabbit aorta in vitro.
|
Oryctolagus cuniculus
|
3.311
nM
|
|
|
pA2 value was determined by the compound's ability to antagonize the AII-induced contraction of rabbit aorta rings.
|
Oryctolagus cuniculus
|
3.802
nM
|
|
|
Inhibition of angiotensin II induced contractions in rabbit aortic ring preparation.
|
Oryctolagus cuniculus
|
1.585
nM
|
|
|
Inhibition of all induced contractions of rabbit aortic rings
|
Oryctolagus cuniculus
|
24.0
nM
|
|
|
Compound was evaluated for antagonism of angiotensin II induced contraction of rabbit aorta rings.
|
Oryctolagus cuniculus
|
7.943
nM
|
|
|
Inhibition of angiotensin II induced contraction in rabbit aortic strips after 60 minutes contact with the compound
|
Oryctolagus cuniculus
|
9.9
nM
|
|
|
Antagonistic activity through inhibition of A II induced contractions on rabbit aortic strips
|
Oryctolagus cuniculus
|
25.0
nM
|
|
|
In vitro antagonist activity was determined by the ability to antagonize the contractile response to angiotensin II in the isolated rabbit aortic strips
|
Oryctolagus cuniculus
|
6.1
nM
|
|
|
Tested in vivo for inhibition of pressor response induced by infusion of AII in conscious normotensive rats, when given intravenously
|
Rattus norvegicus
|
0.65
mg kg-1
|
|
|
In vitro antagonistic activity by displacement of [125I]-Sar1-Ile8-A II at the rat adrenal cortical aorta AT1 receptor
|
Rattus norvegicus
|
19.0
nM
|
|
|
Percent inhibition of angiotensin II (0.1 ug/kg iv) -induced pressor response 3h after administration of test compounds (1 mg/kg po) in conscious male Sprague-Dawley rats
|
None
|
21.0
%
|
|
|
Percent inhibition of angiotensin II (0.1 ug/kg iv) -induced pressor response 7 hr after administration of test compounds (1 mg/kg po) in conscious male Sprague-Dawley rats
|
None
|
34.0
%
|
|
|
Percent inhibition of AII vasopressor response in SHR at 5 mg/kg of oral dose after 5 hr in hypertensive rats
|
Rattus norvegicus
|
50.0
%
|
|
|
In vivo inhibitory activity against pressor response induced by exogenously administered angiotensin-II (0.1 ug/kg, i.v.) in rat at dose 1 mg/kg after intravenous administration
|
Rattus norvegicus
|
78.0
%
|
|
|
In vivo inhibitory percentage of pressor response induced by exogenous submaximal dose of angiotensin -II (1 mg/kg) administered iv to pithed rats
|
Rattus norvegicus
|
62.5
%
|
|
|
In vivo inhibitory percentage of pressor response induced by exogenous submaximal dose of angiotensin -II (3 mg/kg) administered iv to pithed rats
|
Rattus norvegicus
|
93.5
%
|
|
|
In vivo inhibition of AII pressor response was measured in conscious, normotensive rats after intravenous administration at dose 1.0 mg/kg
|
Rattus norvegicus
|
78.0
%
|
|
|
In vivo inhibition of AII pressor response was measured in conscious, normotensive rats after po administration at dose 3.0 mg/kg
|
Rattus norvegicus
|
94.0
%
|
|
|
Inhibition of AII pressor response expressed as peak inhibition in conscious normotensive rats at 1 mg/Kg i.v.
|
Rattus norvegicus
|
78.0
%
|
|
|
Inhibition of AII pressor response expressed as peak inhibition in conscious normotensive rats at 1 mg/Kg p.o.
|
Rattus norvegicus
|
58.0
%
|
|
|
Inhibition of AII pressor response expressed as peak inhibition in conscious normotensive rats at 3 mg/Kg p.o.
|
Rattus norvegicus
|
94.0
%
|
|
|
Inhibitory activity against the pressor response induced by angiotensin II (AII) in conscious rats, at 1 mg/kg p.o. at 3h
|
Rattus norvegicus
|
21.0
%
|
|
|
Inhibitory activity against the pressor response induced by angiotensin II (AII) in conscious rats, at 1 mg/kg p.o. at 7 hr
|
Rattus norvegicus
|
34.0
%
|
|
|
Inhibitory activity against AII-Induced Pressor response at 1 mg/Kg at 1 hr
|
Rattus norvegicus
|
12.0
%
|
|
|
Inhibitory activity against AII-Induced Pressor response at 1 mg/Kg at 3 hour
|
Rattus norvegicus
|
12.0
%
|
|
|
Inhibitory activity against AII-Induced Pressor response at 1 mg/Kg at 6 hour
|
Rattus norvegicus
|
32.0
%
|
|
|
Inhibitory activity against AII-Induced Pressor response at 10 mg/Kg at 1 hr
|
Rattus norvegicus
|
69.0
%
|
|
|
Inhibitory activity against AII-Induced Pressor response at 10 mg/Kg at 3 hour
|
Rattus norvegicus
|
77.0
%
|
|
|
Inhibitory activity against AII-Induced Pressor response at 10 mg/Kg at 6 hour
|
Rattus norvegicus
|
85.0
%
|
|
|
Inhibitory activity against AII-Induced Pressor response at 3 mg/Kg at 1 hr
|
Rattus norvegicus
|
38.0
%
|
|
|
Inhibitory activity against AII-Induced Pressor response at 3 mg/Kg at 3 hour
|
Rattus norvegicus
|
35.0
%
|
|
|
Inhibitory activity against AII-Induced Pressor response at 3 mg/Kg at 6 hour
|
Rattus norvegicus
|
65.0
%
|
|
|
Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 2 h.
|
None
|
12.0
%
|
|
|
Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 24 h.
|
None
|
17.0
%
|
|
|
Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 3 h.
|
None
|
21.0
%
|
|
|
Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 5 h.
|
None
|
35.0
%
|
|
|
Inhibitory activity on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 7 h.
|
None
|
34.0
%
|
|
|
Inhibitory activity on AII (100 ng/kg iv)-induced pressor response at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 1 h.
|
None
|
1.0
%
|
|
|
In vivo concentration inhibiting angiotensin II (A II) induced pressor response in conscious normotensive rats 30 mins after oral administration of 2 uM/kg.
|
Rattus norvegicus
|
-33.0
%
|
|
|
Inhibitory effect on AII (100 ng/kg iv)-induced pressor response after administration at 0.1 mg/kg po in conscious male Sprague-Dawley rats at 0.5 h.
|
None
|
5.0
%
|
|
|
Maximum percent change in A II supported mean arterial pressure 60 minutes following 3 mg/kg i.d. administration.
|
Rattus norvegicus
|
-72.0
%
|
|
|
Peak percent inhibition of Angiotensin II pressor response in conscious, normotensive rats at 0.3 mg/kg iv (no. of animals treated)
|
Rattus norvegicus
|
52.0
%
|
|
|
Peak percent inhibition of Angiotensin II pressor response in conscious, normotensive rats at 0.3 mg/kg po (no. of animals treated)
|
Rattus norvegicus
|
36.0
%
|
|
|
Peak percent inhibition of Angiotensin II pressor response in conscious, normotensive rats at 1 mg/kg iv (no. of animals treated)
|
Rattus norvegicus
|
78.0
%
|
|
|
Peak percent inhibition of Angiotensin II pressor response in conscious, normotensive rats at 3 mg/kg po (no. of animals treated)
|
Rattus norvegicus
|
94.0
%
|
|
|
Tested for inhibition of Angiotensin II-induced pressor response in pithed rat model after 10 mg/kg peroral administration
|
Rattus norvegicus
|
50.0
%
|
|
|
Percent peak inhibition of pressor response induced by exogenously administered AII (submaximal dose (mg/kg) ) in groups of 2 or more pithed rats.
|
Rattus norvegicus
|
62.5
%
|
|
|
Percent peak inhibition of pressor response induced by exogenously administered AII at 3 mg/kg in 2 or more pithed rats.
|
Rattus norvegicus
|
93.5
%
|
|
|
The compound was evaluated for the percentage of inhibition of A II pressor response in rat for intravenous administration
|
Rattus norvegicus
|
0.28
%
|
|
|
The compound was evaluated for the percentage of inhibition of A II pressor response in rat for peroral administration.
|
Rattus norvegicus
|
0.66
%
|
|
|
Inhibition of AII pressor response by the compound in conscious, normotensive rats, at 0.3 (mg/kg) intravenous dose
|
Rattus norvegicus
|
52.0
%
|
|
|
Inhibition of AII pressor response by the compound in conscious, normotensive rats, at 1 (mg/kg) intravenous dose
|
Rattus norvegicus
|
78.0
%
|
|
Inhibition of AII pressor response by the compound in conscious, normotensive rats, at 1 (mg/kg) intravenous dose
|
Rattus norvegicus
|
78.0
%
|
|
|
Inhibition of AII pressor response by the compound in conscious, normotensive rats, at 1 (mg/kg) peroral dose
|
Rattus norvegicus
|
58.0
%
|
|
|
Inhibition of AII pressor response by the compound in conscious, normotensive rats, at 3 (mg/kg) intravenous dose
|
Rattus norvegicus
|
94.0
%
|
|
|
Peak inhibition of A II pressor response in conscious normotensive rats after intravenous administration of 0.3 mg/kg of drug (4 animals treated)
|
Rattus norvegicus
|
52.0
%
|
|
|
Peak inhibition of A II pressor response in conscious normotensive rats after peroral administration of 0.3 mg/kg of drug (2 animals treated)
|
Rattus norvegicus
|
36.0
%
|
|
|
Peak inhibition of A II pressor response in conscious normotensive rats after peroral administration of 3 mg/kg of drug (4 animals treated)
|
Rattus norvegicus
|
94.0
%
|
|
|
In vivo inhibitory activity against pressor response induced by exogenously administered angiotensin-II (0.1 ug/kg, i.v.) in monkey at dose 1 mg/kg after intravenous administration
|
Cercopithecidae
|
76.0
%
|
|
|
In vivo inhibitory activity against pressor response induced by exogenously administered angiotensin-II (0.1 ug/kg, i.v.) in anesthetized chimpanzee at dose 1 mg/kg after 10 hours of intravenous administration
|
Pan troglodytes
|
44.0
%
|
|
|
In vivo inhibitory activity against pressor response induced by exogenously administered angiotensin-II (0.1 ug/kg, i.v.) in anesthetized chimpanzee at dose 1 mg/kg after 24 hours of intravenous administration
|
Pan troglodytes
|
13.0
%
|
|
|
In vivo inhibitory activity against pressor response induced by exogenously administered angiotensin-II (0.1 ug/kg, i.v.) in anesthetized chimpanzee at dose 1 mg/kg after 3 hours of intravenous administration
|
Pan troglodytes
|
66.0
%
|
|
|
In vitro antagonistic potency against angiotensin II receptor using [125I]- Sar,Ile8-angiotensin II as the radioligand in rat adrenal cortical membranes
|
None
|
95.0
nM
|
|
|
Displacement of [125I]-Ang II from rat liver membrane angiotensin II type 1 (AT1) receptor
|
Rattus norvegicus
|
1.9
nM
|
|
|
Competitive antagonism of Angiotensin II receptor in endothelium removed isolated rat aortic ring; (n = 5)
|
Rattus norvegicus
|
39.81
nM
|
|
|
Displacement of [125I]-Ang II from rat liver membrane angiotensin II type 1 (AT1) receptor
|
Rattus norvegicus
|
12.1
nM
|
|
|
Displacement of [125I]Sar1,Ile8-Ang2 from AT1 receptor in rat hepatic membrane
|
Rattus norvegicus
|
6.7
nM
|
|
|
Antagonist activity against AT1 receptor assessed as inhibition of Ang2-induced rabbit aortic strip contraction
|
Oryctolagus cuniculus
|
10.0
nM
|
|
|
Displacement of [125I]angiotensin-2 from bovine adrenal cortex AT1 receptor
|
Bos taurus
|
120.0
nM
|
|
|
Antagonist activity at AT1 receptor assessed inhibition of angiotensin-2-induced contraction of rabbit thoracic aortic rings
|
Oryctolagus cuniculus
|
12.59
nM
|
|
|
Displacement of [125I]Sar1,Ile8-Ang2 from AT1 receptor in Wistar rat hepatic membrane
|
Rattus norvegicus
|
6.7
nM
|
|
|
Antagonist activity at AT1 receptor in KCl-contracted rabbit aortic strips after 60 mins
|
Oryctolagus cuniculus
|
199.53
nM
|
|
|
Antagonist activity at HA-tagged mouse AT1a angiotensin 2 receptor expressed in HEK293T cells assessed as decrease in angiotensin 2-induced intracellular calcium uptake
|
None
|
2.4
ug.mL-1
|
|
|
Antagonist activity at AT1 receptor in rat aorta
|
Rattus norvegicus
|
39.81
nM
|
|
|
Displacement of [125I]Ang2 from AT1 receptor in bovine adrenal cortex
|
Bos taurus
|
160.0
nM
|
|
|
Antagonist activity at AT1 receptor in rat aortic rings
|
Rattus norvegicus
|
10.0
nM
|
|
|
Displacement of [125I]angiotensin 2 from AT1 receptor in rat liver membrane after 2 hrs by gamma counting
|
Rattus norvegicus
|
12.1
nM
|
|
|
Antagonist activity at angiotensin AT1 receptor
|
None
|
3.311
nM
|
|
|
Displacement of radiolabeled angiotensin2 from angiotensin AT1 receptor in rat adrenal cortex membranes
|
Rattus norvegicus
|
19.0
nM
|
|
|
Displacement of radiolabeled angiotensin2 from angiotensin AT1 receptor in rat vascular smooth muscle
|
Rattus norvegicus
|
20.0
nM
|
|
|
Antagonist activity at angiotensin AT1 receptor in rat adrenal cortical membranes
|
Rattus norvegicus
|
0.82
nM
|
|
|
Binding affinity to angiotensin AT1 receptor in rat liver membranes
|
Rattus norvegicus
|
6.7
nM
|
|
|
Antagonist activity at angiotensin AT1 receptor in rabbit thoracic aortic rings
|
Oryctolagus cuniculus
|
12.59
nM
|
|
|
Antagonist activity at angiotensin AT1 receptor in rat kidney homogenates
|
Rattus norvegicus
|
15.85
nM
|
|
|
Displacement of [125I]Sar1 Ile8-Ang 2 from angiotensin 2 AT1 receptor after 180 mins by gamma counting
|
None
|
16.2
nM
|
|
|
Antagonist activity at angiotensin 2 AT1 receptor in Japanese White rabbits thoracic aorta assessed as inhibition of KCl-indcuced contraction after 60 mins
|
Oryctolagus cuniculus
|
12.59
nM
|
|
|
Antagonist activity at angiotensin 2 receptor type 1 in New Zealand White rabbit descending thoracic aorta rings assessed as inhibition of angiotensin 2-induced contraction preincubated for 30 mins prior angiotensin 2 challenge
|
Oryctolagus cuniculus
|
61.12
nM
|
|
|
Displacement of [125I]angiotensin 2 from angiotensin 2 receptor type 1 in Sprague-Dawley rat adrenal cortex membranes after 60 mins by gamma counting
|
Rattus norvegicus
|
80.0
nM
|
|
|
Antihypertensive activity against angiotensin-2-induced cell contraction in Wistar rat VSMC assessed as changes in planar cell surface area after 30 mins by planimetric technique
|
Rattus norvegicus
|
93.0
%
|
|
|
Displacement of [125I]AngII from type 1 angiotensin 2 receptor in bovine adrenal cortex
|
Bos taurus
|
95.0
nM
|
|
|
Displacement of [125I]Sar1Ile8-Ang2 from angiotensin AT1 receptor after 180 mins by gamma counting
|
Homo sapiens
|
16.2
nM
|
|
|
Antagonist activity at AT1 receptor in Japanese white rabbit thoracic aorta assessed as inhibition of KCl-induced contraction incubated 30 mins post KCl-induction for 1 hr
|
Oryctolagus cuniculus
|
12.59
nM
|
|
|
Inhibition of angiotensin AT1 receptor
|
Homo sapiens
|
0.33
nM
|
|
|
Displacement of 125[I-Sar1-Ile8]ANG II from human AT1 receptor expressed in HEK293 membranes after 1 hr by gamma counting
|
Homo sapiens
|
5.623
nM
|
|
Displacement of 125[I-Sar1-Ile8]ANG II from human AT1 receptor expressed in HEK293 membranes after 1 hr by gamma counting
|
Homo sapiens
|
6.0
nM
|
|
|
Antagonist activity at AT1 receptor in rat uterus assessed inhibition of oxytocin/bradykinin-induced contraction
|
Rattus norvegicus
|
5.623
nM
|
|
|
Antagonist activity at angiotensin 2 receptor
|
None
|
19.0
nM
|
|
|
Displacement of [125I]Angiotensin-2 from angiotensin AT1 receptor in Sprague-Dawley rat VSMC after 60 mins by gamma counting
|
Rattus norvegicus
|
1.41
nM
|
|
Displacement of [125I]Angiotensin-2 from angiotensin AT1 receptor in Sprague-Dawley rat VSMC after 60 mins by gamma counting
|
Rattus norvegicus
|
1.64
nM
|
|
|
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay
|
Homo sapiens
|
12.0
%
|
|
|
Antagonist activity at Angiotensin 2 type-1 receptor in Wistar rat uterus assessed as suppression of ANG2-induced contraction
|
Rattus norvegicus
|
5.623
nM
|
|
|
Displacement of [125I-Sar1-Ile8]-ANG2 from human Angiotensin 2 type-1 receptor expressed in HEK293 cells after 1 hr by gamma counting analysis
|
Homo sapiens
|
5.623
nM
|
|
|
Antagonist activity at angiotensin-2 receptor in Wistar rat endothelium denuded thoracic aorta assessed as inhibition of angiotensin 2-induced contraction preincubated for 30 mins prior to angiotensin 2-challenge
|
Rattus norvegicus
|
3.715
nM
|
|
|
Antagonist activity at angiotensin 2 receptor in Japanese white rabbit thoracic aorta assessed as inhibition of angiotensin 2-induced contraction after 60 mins by Schild plot analysis
|
Oryctolagus cuniculus
|
12.02
nM
|
|
|
Displacement of [125I]-Sar1Ile8-angiotensin 2 from angiotensin 2 AT1 receptor (unknown origin) after 180 mins by gamma counting analysis
|
Homo sapiens
|
16.2
nM
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
23.21
%
|
|
|
pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells
|
Cricetulus griseus
|
288.4
nM
|
|
|
Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells
|
Cricetulus griseus
|
160.0
nM
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
3.759
%
|
|
|
Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells
|
Cricetulus griseus
|
890.0
nM
|
|
|
Displacement of [125I]-Ang-2 from AT1 receptor in rat liver membranes after 1.5 hrs
|
Rattus norvegicus
|
85.0
nM
|
|
|
Displacement of [125I]-angiotensin 2 from angiotensin AT1 receptor in VSMC of Sprague-Dawley rat thoracic aorta after 60 mins by gamma-counting
|
Rattus norvegicus
|
3.54
nM
|
|
Displacement of [125I]-angiotensin 2 from angiotensin AT1 receptor in VSMC of Sprague-Dawley rat thoracic aorta after 60 mins by gamma-counting
|
Rattus norvegicus
|
2.53
nM
|
|
|
Displacement of [125I]Sar1Ile8-Ang2 from human AT1 receptor expressed in CHO-K1 cell membranes after 180 mins
|
Homo sapiens
|
28.6
nM
|
|
|
Antagonist activity against AT1 receptor in Japanese White rabbit aortic strips assessed as reduction in angiotension-2-induced contractile response after 60 mins by Schild's plot analysis
|
Oryctolagus cuniculus
|
19.95
nM
|
|
|
Displacement of 125I-labelled Sar1-Ile8-angiotensin-2 from human AT1 receptor
|
Homo sapiens
|
16.2
nM
|
|
|
Displacement of 125I-[Sar1,Leu8] angiotensin-2 from rat type 1 angiotensin-2 receptor expressed in African green monkey COS7 cells after 24 hrs
|
Rattus norvegicus
|
12.1
nM
|
|
|
Displacement of [125I]-Ang II from Angiotensin 2 type-1A receptor in rat vascular smooth muscle cells after 150 mins by gamma counting method
|
Rattus norvegicus
|
13.86
nM
|
|
Displacement of [125I]-Ang II from Angiotensin 2 type-1A receptor in rat vascular smooth muscle cells after 150 mins by gamma counting method
|
Rattus norvegicus
|
19.15
nM
|
|
|
Displacement of [3H]-Asp-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-ValTyr-Ile-His-Pro-Phe-OH Tris(hydrotrifluoroacetate) from human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ after 2 hrs by liquid scintillation counting
|
Homo sapiens
|
12.0
nM
|
|
|
Displacement of [3H]-Angiotensin 2 from AT1 receptor in human PLC/PRF/5 cells after 20 mins by liquid scintillation counting
|
Homo sapiens
|
17.0
nM
|
|
|
Displacement of [125I]-Sar1,Ile8-angiotensin 2 from AT1 receptor in Sprague-Dawley rat vascular smooth muscle cells after 150 mins by gamma counting analysis
|
Rattus norvegicus
|
20.09
nM
|
|
Displacement of [125I]-Sar1,Ile8-angiotensin 2 from AT1 receptor in Sprague-Dawley rat vascular smooth muscle cells after 150 mins by gamma counting analysis
|
Rattus norvegicus
|
13.06
nM
|
|
|
Displacement of [125I-Sar1-Ile8]Ang2 from human AT1 receptor expressed in HEK293 cell membrane incubated for 1 hr by gamma counting method
|
Homo sapiens
|
3.236
nM
|
|
|
Blocking activity at AT1 receptor in rat aortic vascular smooth muscle cells assessed as inhibition of angiotensin-2-induced calcium flux at 10 uM preincubated for 20 mins followed by angiotensin-2 addition by Fura-2-AM dye based scanning fluorometric method relative to control
|
Rattus norvegicus
|
78.0
%
|
|
|
Displacement of Europium-labeled angiotensin-2 from human AT1 receptor expressed in CHOK1 cell membranes after 120 mins by DELFIA
|
Homo sapiens
|
5.012
nM
|
|
|
In vivo antagonist activity at AT1 receptor in Sprague-Dawley rat assessed as inhibition of angiotensin-2-induced pressor response at 3 mg/kg, iv treated for 5 mins at 15 mins post 2 doses of angiotensin-2 treatment at 15 minutes apart followed by ANP treatment and subsequent angiotensin-2 re-challenge after 60 mins relative to control
|
Rattus norvegicus
|
67.0
%
|
|
|
Antagonist activity at AT1 receptor (unknown origin) by inositol phosphate accumulation assay relative to control
|
Homo sapiens
|
87.0
%
|
|
|
Inhibition of ATR1 (unknown origin)
|
Homo sapiens
|
350.0
nM
|
|
|
Inhibition of AGE formation assessed as reduction in reduction in bovin serum albumin glycation at 1 mM incubated for 24 hrs in presence of glucose, Cu2+ by spectrophotometric analysis relative to control
|
None
|
51.4
%
|
|
|
Inhibition of Cu2+ ion-induced oxidation of ascorbic acid by spectrophotometric analysis
|
None
|
91.2
%
|
|
|
Inhibition of AGE formation assessed as reduction in bovin serum albumin glycation at 1 mM incubated for 24 hrs in presence of glucose by spectrophotometric analysis relative to control
|
None
|
51.4
%
|
|
|
Inhibition of [125I] Ang2 binding to AT1 receptor in Sprague-Dawley rat VSMC after 150 mins by gamma-counter method
|
Rattus norvegicus
|
14.6
nM
|
|
Inhibition of [125I] Ang2 binding to AT1 receptor in Sprague-Dawley rat VSMC after 150 mins by gamma-counter method
|
Rattus norvegicus
|
10.5
nM
|
|
|
Displacement of [125I]-angiotensin-2 from AT1 receptor in Sprague-Dawley rat vascular smooth muscle cells after 150 mins by gamma counting method
|
Rattus norvegicus
|
14.6
nM
|
|
Displacement of [125I]-angiotensin-2 from AT1 receptor in Sprague-Dawley rat vascular smooth muscle cells after 150 mins by gamma counting method
|
Rattus norvegicus
|
10.5
nM
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
24.92
%
|
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.25
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.25
%
|
|
|
Inhibition of [3H]-U46619 binding to TxA2 receptor in human platelet suspension at 0.7 uM incubated for 30 mins by liquid scintillation counting method relative to control
|
Homo sapiens
|
50.0
%
|
|
