GCGR-IN-17 ( PF-06291874 | PF06291874 | PF-6291874 )

产品货号. M11636 CAS No. 1393124-08-7

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

GCGR-IN-17
注意事项

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
产品简述

一种高效胰高血糖素受体拮抗剂，对 hGCGR 的 Ki 为 14 nM。
产品描述

A highly potent glucagon receptor antagonist with Ki of 14 nM for hGCGR; shows excellent selectivity against a panel of 69 receptors, ion channels, uptake sites and enzymes; reduces the glucagon-elicited glucose excursion in a dose-dep endent manner in rats; displays low in vivo clearance and excellent oral bioavailability in both rats and dogs.Diabetes Phase 2 Discontinued.
体外实验

——
体内实验

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%.
同义词

PF-06291874 | PF06291874 | PF-6291874
通路

GPCR/G Protein
靶点

Glucagon Receptor
受体

Glucagon Receptor
研究领域

Metabolic Disease
适应症

Diabetes

CAS Number

1393124-08-7
分子量

503.5134
分子式

C26H28F3N3O4
纯度

>98% (HPLC)
溶解度

DMSO: ≥ 30 mg/mL
SMILES

O=C(O)CCNC(C1=CC=C([C@@H](OC2=CC(C)=C(C(C)=C2)N3C=C(C=N3)C(F)(F)F)CCC)C=C1)=O
化学全称

glucagon receptor antagonists-4, N-[4-[(1S)-1-[3,5-dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy]butyl]benzoyl]-

1. Guzman-Perez A, et la. Bioorg Med Chem Lett. 2013 May 15;23(10):3051-8.

计算器

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