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GRA Ex-25

CAS No. : 307983-31-9

MCE 国际站：GRA Ex-25

产品活性：GRA Ex-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 55 nM。

研究领域：GPCR/G Protein

作用靶点：Glucagon Receptor

In Vitro: GRA Ex-25 binds a human glucagon receptor (h-GlucRbind) with K_i of 63 nM and a moderate glucagon induced adenylate cyclase inhibition (h-GlucRcyclase) with K_i 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).

In Vivo: 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.

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