GRAEx-25是一种glucagon受体的抑制剂，抑制大鼠和人的glucagon受体，IC50值分别为56和55nM。
CAS：307983-31-9
分子式：C29H36F3N3O5
分子量：563.61
纯度：98%
存储：Store at -20°C

Background:

GRA Ex-25 is an inhibitor of glucagon receptor, with IC50 of 56 and 55 nM for rat and human glucagon receptors, respectively.

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[1]. GRA Ex-25 has similar affinity to the rat and human glucagon receptors (IC50=56 and 55 nM, respectively)[2].

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[2].

[1]. Kurukulasuriya R, et al. Biaryl amide glucagon receptor antagonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2047-50. [2]. Lau J, et al. New beta-alanine derivatives are orally available glucagon receptor antagonists. J Med Chem. 2007 Jan 11;50(1):113-28.