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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-LTGO-33
LTGO-33

Chemical Structure : LTGO-33

CAS No.: 2834106-06-6

LTGO-33 (LTGO33)

货号: PC-21678Not For Human Use, Lab Use Only.

LTGO-33 is a potent, selective inhibitor of voltage-gated sodium channel NaV1.8 with IC50 of 44 nM (hNaV1.8), 600-fold selectivity against NaV1.1-NaV1.7 and NaV1.9.

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

生物&药学活性

LTGO-33 is a potent, selective inhibitor of voltage-gated sodium channel NaV1.8 with IC50 of 44 nM (hNaV1.8), 600-fold selectivity against NaV1.1-NaV1.7 and NaV1.9.
LTGO-33 inhibits TTX-R currents in primary DRG neurons from human and cynomolgus monkey but is markedly less effective on DRG neurons from dog and mouse.
LTGO-33 binds to the extracellular cleft of VSDII, stabilizes the deactivated state of VSDII.
LTGO-33 is state-independent with similar potencies against closed and inactivated channels.
LTGO-33 equally inhibits wild-type and multiple NaV1.8 variants associated with human pain disorders.

物理化学性质&存储条件

分子量 467.44
分子式 C21H17F4N3O3S
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

(R)-2-(4-fluoro-2-methylphenoxy)-N-(3-(S-methylsulfonimidoyl)phenyl)-5-(trifluoromethyl)nicotinamide

参考文献

1. Gilchrist JM, et al. Mol Pharmacol. 2024 Jan 9:MOLPHARM-AR-2023-000789.

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