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Cat. No. Product Name CAS No. Information
PC-42961

GKT137831

1218942-37-0

GKT137831 (Setanaxib, GKT-137831) is a potent, selective, dual NADPH oxidase Nox1/4 inhibitor with Ki of 110/140 nM, 15-fold less potent on Nox2 and 3-fold less potent on Nox5, and no affinity for xanthine oxidase; attenuates liver fibrosis and ROS production in both SOD1mu and WT mice, suppresses ROS production and NOX and fibrotic gene expression, but not Rac1 activity, in SOD1mut and WT in hepatic stellate cells (HSCs).

Diabetes

Phase 2 Clinical

PC-63184

ZGN-1061

2082752-83-6

ZGN-1061 (Aclimostat) is a novel potent, selective Methionine aminopeptidase 2 (MetAP2) inhibitor being investigated for treatment of diabetes and obesity; reduces body weight in diet-induced obese (DIO) insulin-resistant mice, also produced improvements in metabolic parameters, including plasma glucose and insulin, and, in HepG2 cells, initiated gene changes similar to beloranib; does not increase coagulation markers in dogs and ZGN-1061 had a greatly improved safety profile in rats relative to beloranib.

Diabetes

Phase 2 Clinical

PC-62464

O-304

1261289-04-6

O-304 is a small molecule AMPK activator and PCSK9 modulator, reduces extracellular and secreted PCSK9 levels in human liver cells and reduces PCSK9 plasma levels and total cholesterol levels in obese rats.

Diabetes

Phase 2 Clinical

PC-61879

MK-0941 mesylate

1137916-97-2

MK-0941 mesylate (MK0941) is a novel potent, orally active Glucokinase (GK) activator with EC50 of 0.240 and 0.065 uM in 2.5 and 10 mM glucose, respectively; increases insulin secretion by 17-fold and glucose uptake up to 18-fold, respectively, in isolated rat islets of Langerhans and hepatocytes at 10 uM; exhibits strong glucose-lowering activity in rodent models of type 2 diabetes and healthy dogs.

Diabetes

Phase 2 Discontinued

PC-61878

MK-0941

752240-01-0

MK-0941 (MK0941) is a novel potent, orally active Glucokinase (GK) activator with EC50 of 0.240 and 0.065 uM in 2.5 and 10 mM glucose, respectively; increases insulin secretion by 17-fold and glucose uptake up to 18-fold, respectively, in isolated rat islets of Langerhans and hepatocytes at 10 uM; exhibits strong glucose-lowering activity in rodent models of type 2 diabetes and healthy dogs.

Diabetes

Phase 2 Discontinued

PC-61492

BMS-823778

1140898-87-8

BMS-823778 (BMS823778) is an orally available, potent and selective inhibitor of 11βHSD-1 with IC50 of 2.3 nM, displays >10,000-fold selectivity over 11βHSD-2; exhibits robust acute pharmacodynamic effects in cynomolgus monkeys (ED50=0.6mg/Kg) and in diet-induced obese (DIO) mice (ED50=34 mg/Kg), also showed excellent inhibition in an ex vivo adipose DIO mouse model (ED50=5.2 mg/Kg).

Diabetes

Phase 2 Clinical

PC-61451

Mizagliflozin

666843-10-3

Mizagliflozin (DSP-3235, KGA-3235, GSK-1614235) is a potent, selective, orally active SGLT1 inhibitor with Ki of 27 nM, displays >350-fold selectivity over SGLT2; increases stool frequency and loosens stool consistency in phase I study; increases fecal wet weight in a dog model of loperamide-induced constipation and a rat model of low-fiber-diet-induced constipation, similar to lubiprostone.

Diabetes

Phase 1 Clinical

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