GNE-131 是有效的人类钠离子通道 NaV1.7(hNaV1.7)选择性抑制剂,IC50为 3 nM。
产品描述
GNE-131 is a potent and specific inhibitor of human sodium channel NaV1.7 (IC50: 3 nM).
体外活性
GNE-131 shows moderate clearance in human liver microsomes and excellent functional activity against human NaV1.7 (IC50: 0.003 μM).
体内活性
GNE-131 shows low in vivo clearance in dog, rat, and mouse. It also displays excellent efficacy in a transgenic mouse model of induced pain.
Cas No.
1629063-81-5
分子式
C23H30N4O3S
分子量
442.57
储存和溶解度
DMSO:120 mg/mL (271.14 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years