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GRA Ex-25

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Chemical Structure| 307983-31-9 同义名 : -
CAS号 : 307983-31-9
货号 : A387310
分子式 : C29H36F3N3O5
纯度 : 99%+
分子量 : 563.609
MDL号 : MFCD11977277
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(53.23 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Glucagon is the counter-regulatory hormone to insulin that promotes glucose production by stimulating glycogenolysis and gluconeogenesis. Glucagon receptor antagonists are expected to alleviate excessive, uncontrolled glucagon action. GRA Ex-25 is a glucagon receptor antagonist with IC50 values of 55 and 56nM for human and rat glucagon receptors, respectively[2]. GRA Ex-25 moderately inhibits adenylate cyclase activity induced by glucagon with a Ki value of 254nM[3]. The oral availability of GRA Ex-25 in rats was 17% and the in vivo t1/2 value was 90min. Intravenous administration of rats with GRA Ex-25 at a dose of 3mg/kg significantly reduced blood glucose caused by exogenous administration of glucagon (3μg/kg)[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.87mL

1.77mL

0.89mL

17.74mL

3.55mL

1.77mL
参考文献

[1]Kurukulasuriya R, Sorensen BK, et al. Biaryl amide glucagon receptor antagonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2047-50.

[2]Lau J, Behrens C, Sidelmann UG, et al. New beta-alanine derivatives are orally available glucagon receptor antagonists. J Med Chem. 2007;50(1):113-128.

[3]Kurukulasuriya R, Sorensen BK, Link JT, et al. Biaryl amide glucagon receptor antagonists. Bioorg Med Chem Lett. 2004;14(9):2047-2050.