| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 8 nM (Nav1.7) | ||||||||||||
| 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: | ||||||||||||
| Name | Nav1.7-IN-3 | ||||||||||||
| CAS | 1788872-06-9 | ||||||||||||
| Formula | C17H20ClFN4O2S2 | ||||||||||||
| Molar Mass | 430.95 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |