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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-VX-548
VX-548

Chemical Structure : VX-548

CAS No.: 2649467-58-1

VX-548 (Suzetrigine, VX548)

货号: PC-22639Not For Human Use, Lab Use Only.

VX-548 (Suzetrigine) is a potent, highly selective and orally bioavailable inhibitor of NaV1.8 voltage-gated sodium channel with IC50 of 0.7 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

VX-548 (Suzetrigine) is a potent, highly selective and orally bioavailable inhibitor of NaV1.8 voltage-gated sodium channel with IC50 of 0.7 nM.
VX-548 (Suzetrigine) displays 31,000-fold selectivity over all other NaV subtypes (i.e., NaV1.1 to NaV1.7, and NaV1.9) in recombinant cells.
VX-548 (Suzetrigine) shows subnanomolar potency in primary neurons isolated from human dorsal-root ganglia.
In two phase 2 clinical trials of postoperative pain, as compared with placebo, the highest dose, but not lower doses, of VX-548 reduced pain over a 48-hour period.

物理化学性质&存储条件

分子量 473.40
分子式 C21H20F5N3O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((2R,3S,4S,5R)-3-(3,4-Difluoro-2-methoxyphenyl)-4,5-dimethyl-5-(trifluoromethyl)tetrahydrofuran-2-carboxamido)picolinamide

参考文献

1. Jones J, et al. N Engl J Med. 2023 Aug 3;389(5):393-405.

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