PF-06305591 ( PF06305591 | PF 06305591 )

产品货号. M11932 CAS No. 1449473-97-5

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

PF-06305591
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

PF-06305591 (PF06305591) 是一种有效的、高选择性的 NaV1.8 阻断剂，IC50 为 15 nM，对其他钠通道亚型、K+ 通道和 Ca2+ 通道没有显着活性。
产品描述

PF-06305591 (PF06305591) is a potent, highly selective selective NaV1.8 blocker with IC50 of 15 nM, displays no significant activity against other sodium channel subtypes, K+ channels and Ca2+ channels; displays excellent preclinical in vitro ADME and safety profile.Pain Phase 1 Discontinued.
体外实验

PF-06305591 (compound 9) has a highly attractive profile with respect to NaV selectivity, hERG activity, passive permeability and in vitro metabolic stability.
体内实验

PF-06305591 (compound 9) has good rat bioavailability. PF-06305591 offers the possibility of investigating higher IC50 multiples of Nav1.8 blockade in the clinic, and therefore a more thorough evaluation of the role of NaV1.8 in the treatment of pain.
同义词

PF06305591 | PF 06305591
通路

Membrane Transporter/Ion Channel
靶点

Sodium Channel
受体

Sodium Channel
研究领域

Neurological Disease
适应症

Pain

CAS Number

1449473-97-5
分子量

274.368
分子式

C15H22N4O
纯度

>98% (HPLC)
溶解度

In Vitro:?DMSO : 140 mg/mL (510.28 mM)
SMILES

CC(C(C1=NC2=C(N1)C=C(C=C2)C(C)(C)C)N)C(=O)N
化学全称

(2R,3S)-3-amino-3-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)-2-methylpropanamide

1. Brown AD, et al. Bioorg Med Chem. 2019 Jan 1;27(1):230-239.

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