Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC 50 of 8 nM. Pain relief. Limited CNS penetration.
性状
Solid
IC50 & Target[1][2]
IC50: 8 nM (Nav1.7)
体内研究(In Vivo)
Nav1.7-IN-3 (compound 5) shows excellent potency, selectivity, behavioral efficacy in a rodent pain model (30 mg/kg, oral, 35 minutes), and efficacy in a mouse itch model (30 mg/kg, oral, 30 minutes). has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Roecker AJ, et al. Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice. Bioorg Med Chem Lett. 2017 May 15;27(10):2087-2093.
溶解度数据
In Vitro: DMSO : < 1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble or slightly soluble)