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ChemicalBook--->CAS DataBase List--->1788872-06-9

1788872-06-9

1788872-06-9 Structure

1788872-06-9 Structure
IdentificationBack 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 PropertiesBack 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 InformationBack 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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