PF-06291874 (Synonyms: Glucagon receptor antagonists-4)
目录号: PL04982 纯度: ≥99%
CAS No. :1393124-08-7
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中文名称
PF-06291874
中文别名
N-[4-[(1S)-1-[3,5-二甲基-4-[4-(三氟甲基)-1H-吡唑-1-基]苯氧基]丁基]苯甲酰基]-beta-丙氨酸
英文名称
PF-06291874
英文别名
glucagon receptor antagonists-4;N-[4-[(1S)-1-[3,5-Dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy]butyl]benzoyl]--alanine;PF-06291874;CGY4I8F278;(S)-3-(4-(1-(3,5-dimethyl-4-(4-(trifluoromethyl)-1H-pyrazol-1-yl)phenoxy)butyl)benzamido)propanoic acid;BDBM50433577;DB15065;PF06291874; Glucagon receptor antagonists-4;3-[[4-[(1S)-1-[3,5-dimethyl-4-[4-(trifluoromethyl)pyrazol-1-yl]phenoxy]butyl]benzoyl]amino]propanoic acid;beta-Alanine, N-(4-((1S
Cas No.
1393124-08-7
分子式
C26H28F3N3O4
分子量
503.51
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
PF-06291874 是一个口服有效的胰高血糖素受体 的非肽类拮抗剂。PF-06291874 正用于 2 型糖尿病 (T2DM) 的研究。
生物活性
PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM).
性状
Solid
体内研究(In Vivo)
PF-06291874 exposure is approximately dose-proportional with a half-life of ~19.7-22.7 h. PF-06291874 has a fast on and off rate. PF-06291874 is highly bound to human plasma protein, with a mean free fraction of ~0.55%. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (198.61 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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