Chemical Structure : LTGO-33
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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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.
分子量 | 467.44 | |
分子式 | C21H17F4N3O3S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Gilchrist JM, et al. Mol Pharmacol. 2024 Jan 9:MOLPHARM-AR-2023-000789.
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