GCGR antagonist 2,280134-25-0

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GCGR antagonist 2

CAS No. : 280134-25-0

MCE 国际站：GCGR antagonist 2

产品活性：GCGR antagonist 2 是一种呋喃-2-碳酰肼化合物，是具有口服活性的胰高血糖素受体拮抗剂。GCGR antagonist 2 与 hGluR 结合的 K_d 值为 2.3 nM，抑制大鼠受体的 IC₅₀ 值为 0.43 nM。GCGR antagonist 2 可抑制胰高血糖素刺激的糖原分解。

研究领域：GPCR/G Protein

作用靶点：GCGR

In Vitro: GCGR antagonist 2 (compound 74) (25 nM, 250 nM, and 2500 nM; 70 min) inhibits 5 nM glucagon-induced glycogenolysis in primary rat hepatocytes, with an IC₅₀ value of 160 nM.
GCGR antagonist 2 (25 nM, 250 nM, and 2500 nM; 60 min) inhibits glucagon-stimulated cAMP level with the recombinant human glucagon receptor in BHK cells.
GCGR antagonist 2 (1 nM, 10 nM, and 100 nM; 60 min) inhibits glucagon-stimulated cAMP level with isolated rat liver glucagon receptor in BHK cells.

In Vivo: GCGR antagonist 2 (0.5 mg/kg for IV, or 2 mg/kg for PO; single dose) shows mean half-lives of 1.11 h and 1.40 h, respectively.
GCGR antagonist 2 (0 mg/kg, 3 mg/kg, and 10 mg/kg; p.o.) at least partly, inhibits the action of the endogenous glucagon responsible for maintenance of euglycemia in glucagon-challenged Sprague-Dawley rats.

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