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Nav1.7-IN-8

Catalog No. T38911 CAS 1432913-44-4

Synonyms: Nav1.7-IN-8

Nav1.7-IN-8 is a highly potent and selective inhibitor of NaV1.7, exhibiting greater selectivity for inhibiting NaV1.7 compared to the subtypes hNaV1.1 and hNaV1.5. Additionally, Nav1.7-IN-8 has inhibitory effects on CYP2C9 and CYP3A4, with IC50 values of 0.17 μM and 0.077 μM, respectively. Notably, Nav1.7-IN-8 demonstrates significant analgesic properties in rodent models of both acute and inflammatory pain.

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Nav1.7-IN-8, CAS 1432913-44-4

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25 mg	Inquiry	$ 1,520.00

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Description	Nav1.7-IN-8 is a highly potent and selective inhibitor of NaV1.7, exhibiting greater selectivity for inhibiting NaV1.7 compared to the subtypes hNaV1.1 and hNaV1.5. Additionally, Nav1.7-IN-8 has inhibitory effects on CYP2C9 and CYP3A4, with IC50 values of 0.17 μM and 0.077 μM, respectively. Notably, Nav1.7-IN-8 demonstrates significant analgesic properties in rodent models of both acute and inflammatory pain.
Targets&IC50	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, administered intraperitoneally (i.p.) at doses ranging from 0 to 100 mpk for one hour, significantly reduces the pain response during phase 2a of the formalin assay in both rats and mice in a dose-dependent manner. Furthermore, when administered at 10 to 100 mpk over two days, it demonstrates a consistent dose-dependent decrease in pain response across these animal models, indicating its potential as an effective analgesic[1].

Synonyms	Nav1.7-IN-8
Molecular Weight	535.92
Formula	C21H12ClF2N5O4S2
CAS No.	1432913-44-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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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Keywords

Nav1.7-IN-8 1432913-44-4 Nav-1.7-IN-8 Nav1.7 IN 8 Nav1.7IN8 inhibitor inhibit

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