PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC 50 of 15 nM. An excellent preclinical in vitro ADME and safety profile.
性状
Solid
IC50 & Target[1][2]
Nav1.8 1.5 nM (IC50)
体外研究(In Vitro)
PF-06305591 (compound 9) has a highly attractive profile with respect to NaV selectivity, hERG activity, passive permeability and in vitro metabolic stability. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
PF-06305591 (compound 9) has good rat bioavailability. PF-06305591 offers the possibility of investigating higher IC 50 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (322.18 mM; Need ultrasonic)配制储备液