AZD-3161 ( AZD3161 )

产品货号. M11520 CAS No. 1369501-46-1

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

AZD-3161
注意事项

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
产品简述

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。
产品描述

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

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.
体内实验

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).
同义词

AZD3161
通路

Membrane Transporter/Ion Channel
靶点

Sodium Channel
受体

Sodium Channel
研究领域

Neurological Disease
适应症

Pain

CAS Number

1369501-46-1
分子量

459.56
分子式

C26H25N3O3S
纯度

>98% (HPLC)
溶解度

——
SMILES

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

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

1. Bagal SK, et al. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3690-9.

计算器

产品手册

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