Name | Nav1.7-IN-3 |
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Description | Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration[1]. |
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Related Catalog | |
Target |
IC50: 8 nM (Nav1.7)[1] |
In Vivo | Nav1.7-IN-3 (compound 5) shows excellent potency, selectivity, behavioral efficacy in a rodent pain model (30 mg/kg, oral, 35 minutes), and efficacy in a mouse itch model (30 mg/kg, oral, 30 minutes)[1]. Animal Model: C57BL/6 male mice (n=8/group, 25-30g) Dosage: 1, 3, and 10 mg/kg Administration: Oral (0-35 mintues) Result: Nav1.7-IN-3 demonstrates statistically significant, dose-dependent reversal of these effects in the acute phase of the experiment (0-5 min period post formalin injection) and the tonic phase of the experiment (20-35 min period post formalin injection) with full reversal of formalin effects in the tonic phase[1] |
References |
Molecular Formula | C17H20ClFN4O2S2 |
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Molecular Weight | 430.95 |