PF-06305591

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

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。

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.

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

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.

PF06305591 | PF 06305591

Membrane Transporter/Ion Channel

Sodium Channel

Sodium Channel

Neurological Disease

Pain

1449473-97-5

274.368

C15H22N4O

>98% (HPLC)

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

CC(C(C1=NC2=C(N1)C=C(C=C2)C(C)(C)C)N)C(=O)N

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

(-20℃)

With Ice Pack

≥ 2 years