Nav1.7-IN-8 

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].

Nav1.7-IN-8 plasma protein binding is very high in rat with a free fraction of ∼1.1 %^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

535.93

C₂₁H₁₂ClF₂N₅O₄S₂

1432913-44-4

O=S(NC1=NC=NS1)(C2=C(F)C=C(OC3=C(C4=CC=C5ON=C(C5=C4)N)C=C(Cl)C=C3)C(F)=C2)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]