|
Percent inhibition of glucose rise, following 100 mg/kg oral dose in fasted nondiabetic rats
|
Rattus norvegicus
|
41.0
%
|
|
|
Inhibition of DPP4 at 10 mM
|
None
|
12.7
%
|
|
|
Inhibition of DPP4 at 30 mM
|
None
|
21.9
%
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
19.6
%
|
|
|
Antihyperglycemic activity in rat sucrose loaded model assessed as reduction of blood glucose level at 100 mg/kg, po
|
Rattus norvegicus
|
42.0
%
|
|
|
Antihyperglycemic activity in rat streptozotocin-induced diabetic model assessed as reduction of blood glucose level at 100 mg/kg, po after 5 hrs
|
Rattus norvegicus
|
28.0
%
|
|
|
Antihyperglycemic activity in rat streptozotocin-induced diabetic model assessed as reduction of blood glucose level at 100 mg/kg, po after 24 hrs
|
Rattus norvegicus
|
29.8
%
|
|
|
Antihyperglycemic activity in Charles Foster/Wistar albino rat assessed as reduction in blood glucose level at 100 mg/kg, po administered 30 mins before sucrose challenge
|
Rattus norvegicus
|
12.9
%
|
|
|
Antihyperglycemic activity against sucrose challenged streptozotocin-induced diabetic Sprague-Dawley albino rat assessed as reduction in blood glucose level at 100 mg/kg, po administered 30 mins before sucrose challenge measured after 5 hrs
|
Rattus norvegicus
|
19.1
%
|
|
|
Antihyperglycemic activity against sucrose challenged streptozotocin-induced diabetic Sprague-Dawley albino rat assessed as reduction in blood glucose level at 100 mg/kg, po administered 30 mins before sucrose challenge measured after 24 hrs
|
Rattus norvegicus
|
20.2
%
|
|
|
Antihyperglycemic activity in C57BL/Ks db/db mouse assessed as reduction in blood glucose level measured after 3 days relative to control
|
Mus musculus
|
11.2
%
|
|
|
Increase in glucose consumption in insulin-resistant human HepG2 cells after 24 hrs
|
Homo sapiens
|
270.0
nM
|
|
|
Inhibition of mammosphere formation in human MDA-MB-231 cells at 5 mM after 7 days by inverted phase-contrast microscopy
|
Homo sapiens
|
41.4
%
|
|
|
Inhibition of mammosphere formation in human MDA-MB-231 cells at 10 mM after 7 days by inverted phase-contrast microscopy
|
Homo sapiens
|
67.6
%
|
|
|
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting
|
Homo sapiens
|
-3.3
%
|
|
|
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
19.6
%
|
|
|
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
-4.5
%
|
|
|
Inhibition of PTP1B in Rattus norvegicus (rat) L6 cells assessed as cellular 2-deoxy-D-[U-14C]glucose uptake at 500 uM after 18 hr relative to control
|
Rattus norvegicus
|
30.2
%
|
|
|
Inhibition of PTP1B in Rattus norvegicus (rat) L6 cells assessed as increase in 2-deoxy-D-[U-14C]-glucose uptake at 100 uM after 18 hr relative to control
|
Rattus norvegicus
|
30.2
%
|
|
|
Inhibition of PTP1B in Rattus norvegicus (rat) L6 cells assessed as glucose uptake at 50 uM
|
Rattus norvegicus
|
30.2
%
|
|
|
Antihyperglycemic activity in db/db mouse assessed as inhibition of post prandial blood glucose level at 100 mg/kg, po qd administered 15 days by OGTT relative to vehicle-treated control
|
Mus musculus
|
29.7
%
|
|
|
Antihyperglycemic activity in db/db mouse assessed as inhibition of post prandial blood glucose level at 100 mg/kg, po qd administered 15 days measured on day 10 by OGTT relative to vehicle-treated control
|
Mus musculus
|
29.1
%
|
|
|
Antidiabetic activity in Sprague-Dawley albino rat assessed as inhibition of blood glucose level at 300 mg/kg, ip administered 10 mins prior to oral glucose challenge measured after 10 mins by glucometer relative to control
|
Rattus norvegicus
|
57.1
%
|
|
|
Inhibition of gluconeogenesis in Sprague-Dawley rat hepatocytes assessed as decrease in glucose output at 2 mM after 4 hrs by colorimetric assay relative to control
|
Rattus norvegicus
|
75.0
%
|
|
|
Antihyperglycemic activity in Sprague-Dawley rat hepatocytes assessed as inhibition of glucose production at 2 mM after 6 hrs by glucose oxidase activity assay
|
Rattus norvegicus
|
25.0
%
|
|
|
Hypoglycemic activity in diabetic rat model assessed as decrease in blood glucose level at 100 mg/kg, ig administered for 12 days measured on third day of compound dosing by glucometer relative to control
|
Rattus norvegicus
|
7.86
%
|
|
|
Hypoglycemic activity in diabetic rat model assessed as decrease in blood glucose level at 100 mg/kg, ig administered for 12 days measured on sixth day of compound dosing by glucometer relative to control
|
Rattus norvegicus
|
7.86
%
|
|
|
Hypoglycemic activity in diabetic rat model assessed as decrease in blood glucose level at 100 mg/kg, ig administered for 12 days measured on ninth day of compound dosing by glucometer relative to control
|
Rattus norvegicus
|
7.86
%
|
|
|
Hypoglycemic activity in diabetic rat model assessed as decrease in blood glucose level at 100 mg/kg, ig administered for 12 days measured on twelfth day by glucometer relative to control
|
Rattus norvegicus
|
7.86
%
|
|
|
Antidiabetic activity in overnight fasted STZ-induced albino Sprague-Dawley rat diabetic model assessed as decrease in blood glucose level at 100 mg/kg, po measured up to 5 hrs
|
Rattus norvegicus
|
25.9
%
|
|
|
Antidiabetic activity in overnight fasted STZ-induced albino Sprague-Dawley rat diabetic model assessed as decrease in blood glucose level at 100 mg/kg, po measured up to 24 hrs
|
Rattus norvegicus
|
36.0
%
|
|
|
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
|
Homo sapiens
|
11.1
%
|
|
|
Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
Homo sapiens
|
9.9
nM
|
|
|
Cytotoxicity against human PC-3 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
Homo sapiens
|
189.0
nM
|
|
|
Antioxidant activity in STZ-induced diabetic Kunming mouse assessed as reduction in liver MDA level at 80 mg/kg, po administered daily via gavage for 8 weeks and measured at 6 hrs post-final drug dose relative to STZ-treated group
|
Mus musculus
|
43.0
%
|
|
|
Reno-protective activity in STZ-induced Kunming mouse model of diabetes assessed as reduction in urinary total protein excretion at 80 mg/kg, po administered daily via gavage for 8 weeks and measured at week 4 relative to control
|
Mus musculus
|
6.0
%
|
|
|
Reno-protective activity in STZ-induced Kunming mouse model of diabetes assessed as reduction in urinary total protein excretion at 80 mg/kg, po administered daily via gavage for 8 weeks and measured at week 6 relative to control
|
Mus musculus
|
41.0
%
|
|
|
Reno-protective activity in STZ-induced Kunming mouse model of diabetes assessed as reduction in urinary total protein excretion at 80 mg/kg, po administered daily via gavage for 8 weeks and measured at week 8 relative to control
|
Mus musculus
|
18.0
%
|
|
|
Inhibition of thrombin-induced platelet aggregation in mouse platelet isolated from C57BL/6J mouse treated at 200 mg/kg, ig twice a day for 7 days by lumi-aggregometer
|
Mus musculus
|
18.5
%
|
|
