| Identification | Back Directory | [Name]
Nav1.7-IN-3 | [CAS]
1788872-06-9 | [Synonyms]
Nav1.7-IN-3
Benzenesulfonamide, 5-chloro-2-fluoro-4-[[(tetrahydro-1H-pyrrolizin-7a(5H)-yl)methyl]amino]-N-2-thiazolyl- | [Molecular Formula]
C17H20ClFN4O2S2 | [MDL Number]
MFCD31813603 | [MOL File]
1788872-06-9.mol | [Molecular Weight]
430.95 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : < 1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble or slightly soluble) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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].
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]. | [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] |
| [IC 50]
Nav1.7: 8 nM (IC50) | [References]
[1]. Roecker AJ, et al. Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice. Bioorg Med Chem Lett. 2017 May 15;27(10):2087-2093. |
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