1. Membrane Transporter/Ion Channel
    Metabolic Enzyme/Protease
  2. Sodium Channel
    Cytochrome P450
  3. Nav1.7-IN-8

Nav1.7-IN-8 

Cat. No.: HY-141547
Handling Instructions

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.

For research use only. We do not sell to patients.

Nav1.7-IN-8 Chemical Structure

Nav1.7-IN-8 Chemical Structure

CAS No. : 1432913-44-4

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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].

IC50 & Target[1]

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].

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

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].

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

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.
Molecular Weight

535.93

Formula

C₂₁H₁₂ClF₂N₅O₄S₂

CAS No.
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Storage

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

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Product Name:
Nav1.7-IN-8
Cat. No.:
HY-141547
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