PF-05190457

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服生物可利用的生长素释放肽受体 (GHSR) 反向激动剂，结合 pKi 为 8.36；在 10 uM 的 CEREP 组中显示出优异的脱靶活性，血清素 5-HT2B 除外 (IC50=3.7 uM)。

A potent, selective, and orally bioavailable ghrelin receptor (GHSR) inverse agonist with binding pKi of 8.36; displays excellent off-target activity in the CEREP panel at 10 uM with exception of serotonin 5-HT2B (IC50=3.7 uM); demonstrates robust increases in glucose-stimulated insulin secretion in human islets.Alcoholism Phase 2 Clinical.

PF-5190457 has a superior balance of ghrelin receptor pharmacology and off-target selectivity.

PF-5190457 has excellent selectivity and demonstrates robust increases in glucose-stimulated insulin secretion in human whole and dispersed islets.

PF05190457 | PF 5190457 | PF5190457

GPCR/G Protein

GHSR

GHSR

Neurological Disease

Alcoholism

1334782-79-4

512.676

C29H32N6OS

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (487.64 mM)

CC1=CC(C2=CC3=C([C@H](N4CC5(CCN(C(CC(N=C6S7)=CN6C=C7C)=O)CC5)C4)CC3)C=C2)=NC=N1

(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

(-20℃)

With Ice Pack

≥ 2 years