网站主页>>>数据中心>>>工艺路线数据>>>Suzetrigine CAS# 2649467-58-1 2-吡啶羧酰胺,4-[[[(2R,3S,4S,5R)-3-(3,4-二氟-2-甲氧基苯基)四氢-4,5-二甲基-5-(三氟甲基)-2-呋喃基]氨基]-

Suzetrigine CAS# 2649467-58-1 2-吡啶羧酰胺,4-[[[(2R,3S,4S,5R)-3-(3,4-二氟-2-甲氧基苯基)四氢-4,5-二甲基-5-(三氟甲基)-2-呋喃基]氨基]-

Suzetrigine, also known as VX-548, is a selective inhibitor of the voltage-gated sodium channel Nav1.7, being developed by Vertex Pharmaceuticals for the treatment of acute and neuropathic pain. It exhibits potent in vitro inhibition of human Nav1.7 with an IC₅₀ in the low nanomolar range (typically reported around 5–10 nM), while showing over 100-fold selectivity over other Nav isoforms such as Nav1.5 and Nav1.4, minimizing cardiac and skeletal muscle off-target effects. In preclinical studies, VX-548 effectively reduced nociceptive signaling in dorsal root ganglion neurons and demonstrated robust antinociceptive activity in rodent pain models.
📌 参考资料/链接:
State-dependent inhibition of Nav1.8 sodium channels by VX-150 and VX-548By: Vaelli, Patric; et alMolecular Pharmacology (2024), 106(6), 298-308

📄 详细内容

CAS No. 2649467-58-1 2-吡啶羧酰胺,4-[[[(2R,3S,4S,5R)-3-(3,4-二氟-2-甲氧基苯基)四氢-4,5-二甲基-5-(三氟甲基)-2-呋喃基]氨基]-Suzetrigine synthetic routes


State-dependent inhibition of Nav1.8 sodium channels by VX-150 and VX-548By: Vaelli, Patric; et alMolecular Pharmacology (2024), 106(6), 298-308
产品链接: CAS No. 2649467-58-1 ››