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PF-06305591 dihydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-06305591 dihydrate图片
包装:5mg
市场价:2700元

产品介绍
PF-06305591dihydrate是一种有效的、高选择性的电压门控钠通道NaV1.8的阻断剂,其IC50值为15nM。具有良好的临床前体外ADME(吸收、分布、代谢和排泄)和安全性。
Canonical SMILESCC(C)(C)C1=CC=C(NC([C@H]([C@@H](C)C(N)=O)N)=N2)C2=C1.[H]O[H].[H]O[H]
分子式C15H26N4O3
分子量310.39
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile[1].

PF-06305591 (compound 9) has a highly attractive profile with respect to NaV selectivity, hERG activity, passive permeability and in vitro metabolic stability[1].

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[1].

[1]. Brown AD, et al. The discovery and optimization of benzimidazoles as selective NaV1.8 blockers for the treatment of pain. Bioorg Med Chem. 2019 Jan 1;27(1):230-239.