AZD-3161 

AZD-3161 is a potent and selective blocker of Na_V1.7 channel, with a pIC₅₀ of 7.1. AZD-3161 can be used for the research of neuropathic and inflammatory pain^[1][2].

pIC50: 7.1 (NaV1.7 channel)^[1]

AZD-3161 (compound 29) is selective for Na_V1.7 over Na_V1.5 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 V_ss (4.2 L/kg)^[1].
AZD-3161 (10 μmol/kg; p.o.) exhibits high oral bioavailability (44%), long half-life (4.8 h) and C_max (0.30 μmol/L)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

474.43

C₂₃H₂₁F₃N₄O₄

1369501-46-1

O=C(C1=CC=C(COCC(F)(F)F)N=C1)N[C@@H]2COC3=CC=CC(C4=NC=C(OC)N=C4)=C3C2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [2]. Bagal SK, et, al. Recent progress in sodium channel modulators for pain. Bioorg Med Chem Lett. 2014 Aug 15; 24(16): 3690-9.  [Content Brief]