Nav1.7-IN-8_product_DataBase

Bioactivity	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].
Invitro	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:
Name	Nav1.7-IN-8
CAS	1432913-44-4
Formula	C21H12ClF2N5O4S2
Molar Mass	535.93
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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