313254-51-2

313254-51-2 structure

Name: ICA 121431
Chemical Name: Benzeneacetamide, α-phenyl-N-[4-[(2-thiazolylamino)sulfonyl]phenyl]
CAS Number: 313254-51-2
Molecular Formula: C₂₃H₁₉N₃O₃S₂
Molecular Weight: 449.545
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
Create Date: 2016-04-12 22:14:31
Modify Date: 2024-01-02 19:23:49
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.IC50 value: 19 nM (rat Nav1.7) [1]Target: rat Nav1.7 inhibitorICA-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.

Name	Benzeneacetamide, α-phenyl-N-[4-[(2-thiazolylamino)sulfonyl]phenyl]
Synonyms	2,2-Diphenyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]acetamide Benzeneacetamide, α-phenyl-N-[4-[(2-thiazolylamino)sulfonyl]phenyl]- ICA-121431

Description	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.IC50 value: 19 nM (rat Nav1.7) [1]Target: rat Nav1.7 inhibitorICA-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.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel Research Areas >> Cardiovascular Disease
References	[1]. McCormack K, et al. Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels. Proc Natl Acad Sci U S A. 2013 Jul 16;110(29):E2724-32.

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302-H319-H413
Precautionary Statements	P305 + P351 + P338
RIDADR	NONH for all modes of transport