GRA Ex-25

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的胰高血糖素受体抑制剂，对大鼠和人胰高血糖素受体的 IC50 分别为 56 和 55 nM。

A potent glucagon receptor inhibitor with IC50 of 56 and 55 nM for rat and human glucagon receptors; binds to human glucagon receptor with Ki of 63 nM, moderately inhibits glucagon induced adenylate cyclase (Ki=254 nM); significantly reduces blood glucose caused by exogenous administration of glucagon in rat model (3 mg/kg, i.v.).Diabetes Preclinical.

GRA Ex-25 binds a human glucagon receptor (h-GlucRbind) with Ki of 63 nM and a moderate glucagon induced adenylate cyclase inhibition (h-GlucRcyclase) with Ki of 254 nM under our assay conditions. GRA Ex-25 has similar affinity to the rat and human glucagon receptors (IC50=56 and 55 nM, respectively).

GRA Ex-25 (3 mg/kg, i.v.) significantly reduces blood glucose caused by exogenous administration of glucagon in rat model. GRA Ex-25 is able to inhibit the rise in blood glucose levels elicited by exogenous administered glucagon, most likely because of the direct inhibition of glucagon stimulated hepatic glucose output.

GRA Ex-25 | GRA Ex 25 | GRA Ex25 | GRAEx-25

GPCR/G Protein

Glucagon Receptor

humanglucagonreceptor|ratglucagonreceptor

Metabolic Disease

Diabetes

307983-31-9

563.6085

C29H36F3N3O5

>98% (HPLC)

DMSO: ≥ 32 mg/mL

C[C@](C1CC[C@H](N(C(NC2C=CC(OC(F)(F)F)=CC=2)=O)CC2C=CC(C(NCCC(O)=O)=O)=CC=2)CC1)(C)C

β-Alanine, N-[4-[[[trans-4-(1,1-dimethylethyl)cyclohexyl][[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]methyl]benzoyl]-

(-20℃)

With Ice Pack

≥ 2 years