2015年6月25日星期四

ICA-121431|Nav1.7 channel inhibitor|DC Chemicals

ICA-121431|Nav1.7 channel inhibitor|DC Chemicals

ICA-121431 is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, but no inhibition on human, monkey and dog Nav1.7.

Product name: ICA-121431  |Cat No. DC8213|Other names: ICA-121431 |Cas: 313254-51-2|Molecule Weight: 449.54526|Molecule Formular: C23H19N3O3S2| Purity: >98%

ICA-121431 is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, but no inhibition on human, monkey and dog Nav1.7.ICA-121431 exhibited a spectrum of inhibitory activity for Nav human channel subtypes; equipotent inhibition of Nav1.3 and Nav1.1, less potent inhibition of Nav1.2, and much weaker inhibition of Nav1.7, Nav1.6, Nav1.4, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM). the unique subtype selective Nav channel inhibitors ICA-121431 and PF-04856264 interact with amino acid residues on an extracellular facing region of the homologous Domain 4 voltage sensor of Nav1.3 or Nav1.7, which is distinct from previously described interaction sites for TTX or local anesthetic-like Nav channel inhibitors.

For research and scientific purpose only, not for human use.

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