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PF-06291874 {[allProObj[0].p_purity_real_show]}

货号:A404945 同义名: glucagon receptor antagonists-4;GCGR Antagonist IV Ambeed 开学季,买赠积分,赢豪礼

Glucagon receptor antagonists-4 is an selective antagonist of glucagon receptor.

PF-06291874 化学结构 CAS号:1393124-08-7
PF-06291874 化学结构
CAS号:1393124-08-7
PF-06291874 3D分子结构
CAS号:1393124-08-7
PF-06291874 化学结构 CAS号:1393124-08-7
PF-06291874 3D分子结构 CAS号:1393124-08-7
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PF-06291874 纯度/质量文件 产品仅供科研

货号:A404945 标准纯度: {[allProObj[0].p_purity_real_show]}
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PF-06291874 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].
体内研究

The pharmacokinetics of PF-06291874 demonstrate a dose-proportional exposure with an elimination half-life ranging between approximately 19.7 and 22.7 hours. Furthermore, this compound rapidly associates with and dissociates from its target, and is predominantly bound to human plasma proteins, exhibiting a minimal free fraction of about 0.55%[3].

PF-06291874 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.

PF-06291874 实验方案

计算器
存储液制备 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

PF-06291874 技术信息

CAS号1393124-08-7
分子式C26H28F3N3O4
分子量 503.513
别名 glucagon receptor antagonists-4;GCGR Antagonist IV;PF-6291874;Glucagon Receptor Antagonist 4
运输蓝冰
存储条件

粉末 Sealed in dry,Room Temperature

液体 -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

动物实验配方
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