1432913-44-4

1432913-44-4 structure

Name: Nav1.7-IN-8
Chemical Name: Nav1.7-IN-8
CAS Number: 1432913-44-4
Molecular Formula: C₂₁H₁₂ClF₂N₅O₄S₂
Molecular Weight: 535.93
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
Create Date: 2021-09-10 11:34:58
Modify Date: 2024-04-09 18:13:33
Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain[1].

Name	Nav1.7-IN-8

Description	Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain[1].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450 Research Areas >> Inflammation/Immunology
Target	CYP2C9:0.17 μM (IC50) CYP3A4:0.077 μM (IC50)
In Vitro	Nav1.7-IN-8 plasma protein binding is very high in rat with a free fraction of ∼1.1 %[1].
In Vivo	Nav1.7-IN-8 (0~100 mpk, i.p.; 1 hour) shows a reduction of the pain response in phase 2a of the formalin assay in a dose dependent manner and produces a substantial inhibition of the pain response[1]. .Nav1.7-IN-8 (10~100 mpk, i.p.; 2 days) displays a dose-dependent reduction of the pain response[1]. Animal Model: Rats[1] Dosage: 0~100 mpk Administration: I.p.; 1 hour Result: Showed a reduction of the pain response in phase 2a of the formalin assay in a dose dependent manner and produced a substantial inhibition of the pain response. Animal Model: Mice[1] Dosage: 10~100 mpk Administration: I.p.; 2 days Result: Displayed a dose-dependent reduction of the pain response.
References	[1]. Focken T, et al. Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models. ACS Med Chem Lett. 2016;7(3):277-282. Published 2016 Jan 19.

Molecular Formula	C₂₁H₁₂ClF₂N₅O₄S₂
Molecular Weight	535.93

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