PF-06291874

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Chemical Structure| 1393124-08-7 同义名 : glucagon receptor antagonists-4; GCGR Antagonist IV; PF-6291874; Glucagon Receptor Antagonist 4
CAS号 : 1393124-08-7
货号 : A404945
分子式 : C26H28F3N3O4
纯度 : 99%+
分子量 : 503.51
MDL号 : MFCD30343861
存储条件：

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(208.53 mM)，配合低频超声助溶，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
生物活性
描述 PF-06291874, characterized as a powerful, orally administered, non-peptide antagonist of the glucagon receptor, is being researched for its potential application in managing type 2 diabetes mellitus (T2DM)[1].[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.93mL

1.99mL

0.99mL

19.86mL

3.97mL

1.99mL
参考文献

[1]Esther C.Y. Lee et al. Identification of a novel conformationally constrained glucagon receptor antagonist. Bioorg Med Chem Lett, 2014 Feb 1, 24(3):839-44.

[2]Derek J Nunez, et al. Glucagon receptor as a drug target: A witches' brew of eye of newt (peptides) and toe of frog (receptors). Diabetes Obes Metab. 2018 Feb;20(2):233-237.

[3]D J Kazierad, et al. Effects of multiple ascending doses of the glucagon receptor antagonist PF-06291874 in patients with type 2 diabetes mellitus. Diabetes Obes Metab. 2016 Aug;18(8):795-802.