AZD-3161

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AZD-3161 是一种有效的选择性钠通道 Nav1.7 阻滞剂，用于治疗伤害性疼痛。

AZD-3161 is a potent and selective sodium channel Nav1.7 blocker for treatment of nociceptive pain. Pain Phase 1 Discontinued.

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.AZD-3161 inhibits Adenosine Transporter (AT) and Cannabinoid B1 (CB1) receptor, with IC50s of 1.8 μM and 5 μM, respectively.

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.AZD-3161 (3 μmol/kg; i.v.) exhibits long half-life (2.2 h) and Vss (4.2 L/kg).AZD-3161 (10 μmol/kg; p.o.) exhibits high oral bioavailability (44%), long half-life (4.8 h) and Cmax (0.30 μmol/L).

AZD3161

Membrane Transporter/Ion Channel

Sodium Channel

Sodium Channel

Neurological Disease

Pain

1369501-46-1

459.56

C26H25N3O3S

>98% (HPLC)

——

CC[C@@H](c1ccccc1)NC(=O)c2c3ccccc3nc(c2NS(=O)(=O)C)c4ccccc4

3-((methylsulfonyl)amino)-2-phenyl-N-((1S)-1-phenylpropyl)-4-quinolinecarboxamide

(-20℃)

With Ice Pack

≥ 2 years