PF-5190457 (Synonyms: PF-05190457)
目录号: PL11626 纯度: ≥98%
CAS No. :1334782-79-4
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中文名称
PF-5190457
英文名称
PF-5190457
英文别名
1-[2-[(1R)-2,3-Dihydro-5-(6-methyl-4-pyrimidinyl)-1H-inden-1-yl]-2,7-diazaspiro[3.5]non-7-yl]-2-(2-methylimidazo[2,1-b]thiazol-6-yl)-ethanone;2-(2-Methylimidazo[2,1-b][1,3]thiazol-6-yl)-1-{2-[(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]non-7-ylethanone;PF 5190457;PF-5190457;FF33NL9U5G;(R)-2-(2-Methylimidazo[2,1-b]thiazol-6-yl)-1-(2-(5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl)-2,7-diazaspiro[3.5]nonan-7-yl)ethan-1-one;1-[2-[(1R)-2,3-Dihydro-5-(6-methyl-4-pyrimidinyl)-1H-inden-1-yl]-2,7-diazaspiro[3,5]non-7-yl]-2-(2-methylimidazo[2,1-b]thiazol-6-yl)ethanone;2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)-1-[2-[(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]nonan-7-y;2-(2-Methylimidazo[2,1-b][1,3]thiazol-6-yl)-1-[2-[(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-ind;2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)-1-[2-[(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-ind;PF-05190457
Cas No.
1334782-79-4
分子式
C29H32N6Os
分子量
512.67
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
PF-5190457 (PF-05190457) 是一种有效,选择性的生长素释放肽受体 (ghrelin receptor) 反向激动剂, pKi 值为 8.36。
生物活性
PF-5190457 (PF-05190457) is a potent and selective ghrelin receptor inverse agonist with a pK i of 8.36.
性状
Solid
IC50 & Target[1][2]
pKi: 8.36 (Humnan ghrelin receptor)
体外研究(In Vitro)
PF-5190457 has a superior balance of ghrelin receptor pharmacology and off-target selectivity. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
PF-5190457 has excellent selectivity and demonstrates robust increases in glucose-stimulated insulin secretion in human whole and dispersed islets. 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]. Bhattacharya SK, et al. Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate. ACS Med Chem Lett. 2014 Feb 24;5(5):474-9.
溶解度数据
In Vitro: DMSO : 250 mg/mL (487.64 mM; Need ultrasonic)Ethanol : 100 mg/mL (195.06 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

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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