TAK-875|2mg|K1329-上海高创化学科技有限公司

TAK-875

参考价：¥1518

供货周期：

一周

品牌：

规格：

2mg

货号：

K1329

CAS号：

1374598-80-7

SKU:K1329		M. Wt:533.63
Formula:C29H32O7S.1/2H2O		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:1374598-80-7		Synonyms:N/A
Chemical NameN/A

Description	TAK-875
Targets	GPR40
IC50	14 nM(EC50)
In vitro	TAK-875 is a selective G-protein-coupled receptor 40 agonist in development for the treatment of type 2 diabetes mellitus. In rat insulinoma INS-1 833/15 cells, TAK-875 increased intracellular inositol monophosphate and calcium concentration, consistent with activation of the Gqalpha signaling pathway. The insulinotropic action of TAK-875 (10 uM) in INS-1 833/15 and primary rat islets was glucose-dependent.
In vivo	In an oral glucose tolerance test in type 2 diabetic N-STZ-1.5 rats, TAK-875 (1-10 mg/kg p.o.) showed a clear improvement in glucose tolerance and augmented insulin secretion. TAK-875 (10 mg/kg, p.o.) significantly augmented plasma insulin levels and reduced fasting hyperglycemia in male Zucker diabetic fatty rats, whereas in fasted normal Sprague-Dawley rats, TAK-875 neither enhanced insulin secretion nor caused hypoglycemia even at 30 mg/kg.
Clinical Trials	N/A
Features	N/A

Description

TAK-875

Targets

GPR40

IC50

14 nM(EC50)

In vitro

TAK-875 is a selective G-protein-coupled receptor 40 agonist in development for the treatment of type 2 diabetes mellitus. In rat insulinoma INS-1 833/15 cells, TAK-875 increased intracellular inositol monophosphate and calcium concentration, consistent with activation of the Gqalpha signaling pathway. The insulinotropic action of TAK-875 (10 uM) in INS-1 833/15 and primary rat islets was glucose-dependent.

In vivo

In an oral glucose tolerance test in type 2 diabetic N-STZ-1.5 rats, TAK-875 (1-10 mg/kg p.o.) showed a clear improvement in glucose tolerance and augmented insulin secretion. TAK-875 (10 mg/kg, p.o.) significantly augmented plasma insulin levels and reduced fasting hyperglycemia in male Zucker diabetic fatty rats, whereas in fasted normal Sprague-Dawley rats, TAK-875 neither enhanced insulin secretion nor caused hypoglycemia even at 30 mg/kg.

Clinical Trials

N/A

Features

N/A