AZD-3161_product_DataBase

Bioactivity	AZD-3161 is a potent and selective blocker of NaV1.7 channel, with a pIC50 of 7.1. AZD-3161 can be used for the research of neuropathic and inflammatory pain[1][2].
Target	pIC50: 7.1 (NaV1.7 channel)
Invitro	AZD-3161 (compound 29) is selective for NaV1.7 over NaV1.5 and hERG, with pIC50s of 7.1, 4.9 and 4.9, respectively[1].AZD-3161 inhibits Adenosine Transporter (AT) and Cannabinoid B1 (CB1) receptor, with IC50s of 1.8 μM and 5 μM, respectively[1].
In Vivo	AZD-3161 (16-99 μmol/kg; p.o.) displays a dose dependent antinociceptive effect in the phase 1 of the formalin model of pain in rats[1].AZD-3161 (3 μmol/kg; i.v.) exhibits long half-life (2.2 h) and Vss (4.2 L/kg)[1].AZD-3161 (10 μmol/kg; p.o.) exhibits high oral bioavailability (44%), long half-life (4.8 h) and Cmax (0.30 μmol/L)[1].
Name	AZD-3161
CAS	1369501-46-1
Formula	C23H21F3N4O4
Molar Mass	474.43
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Kers I, et, al. Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers. Bioorg Med Chem Lett. 2012 Sep 1; 22(17): 5618-24. [2]. Bagal SK, et, al. Recent progress in sodium channel modulators for pain. Bioorg Med Chem Lett. 2014 Aug 15; 24(16): 3690-9.

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