GRA Ex-25 是glucagon受体抑制剂，其对大鼠和人的 glucagon 受体的IC50值分别为 56 和 55 nM。

GRA-Ex-25 is an inhibitor of glucagon receptor.

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 which is caused by exogenous administration of glucagon in rat models. GRA Ex-25 is able to inhibit the rise in blood glucose levels elicited by exogenously administered glucagon, most likely due to the direct inhibition of glucagon stimulated hepatic glucose output[2].

307983-31-9

C29H36F3N3O5

563.618

GRA-Ex-25

DMSO:32 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years