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NaV1.7 inhibitor 51

Chemical Structure : NaV1.7 inhibitor 51

CAS No.: 2244153-85-1

NaV1.7 inhibitor 51

Catalog No.: PC-72207Not For Human Use, Lab Use Only.

NaV1.7 inhibitor 51 is a highly potent, selective, orally active NaV1.7 inhibitor with IC50 of 10.7 nM in FLIPR membrane potential assay, no significant activity against NaV1.5 (IC50>10 uM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

NaV1.7 inhibitor 51 is a highly potent, selective, orally active NaV1.7 inhibitor with IC50 of 10.7 nM in FLIPR membrane potential assay, no significant activity against NaV1.5 (IC50>10 uM).
NaV1.7 inhibitor 51 shows good selectivity against other NaV isoforms and minimal inhibition at 10 uM for the resting state across different NaV isoforms.
NaV1.7 inhibitor 51 exhibits state-dependent block of human, monkey, and mouse NaV1.7 with a similar potency range.
NaV1.7 inhibitor 51 shows significant effects on the CCI-induced neuropathic pain model.

Physicochemical Properties

M.Wt 499.512
Formula C24H20F3N5O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Month
Shipping
Solubility

Chemical Name/SMILES

References

1. Vidya Ramdas, et al. J Med Chem. 2020 Jun 11;63(11):6107-6133.

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