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AM966

品牌 厂商性质 产地 货期
阿拉丁 生产商 上海 现货

询价
产品参数
货号 CAS号 操作
A125594-10mg 1228690-19-4 询价
A125594-50mg 1228690-19-4 询价
A125594-5mg 1228690-19-4 询价
产品介绍

  • 分子式 C27H23ClN2O5
  • 分子量490.93
  • Beilstein号
  • EC号
  • MDL号
  • PubChem编号

属性

溶解性 DMSO
存贮条件 储存温度-20°C

描述

产品介绍 AM966是高亲和性的口服的溶血磷脂酸(LPA1)受体拮抗剂,IC50为17 nM,比对其它LPA受体的抑制性高。
生化机理

AM966 is a high affinity, selective, oral LPA1 (lysophosphatidic acid receptor) antagonist, with selectivity for this receptor over the other LPA receptors. In vitro, AM966 inhibited LPA-stimulated intracellular calcium release (IC(50)= 17 nM) from Chinese hamster ovary cells stably expressing human LPA(1) receptors and inhibited LPA-induced chemotaxis (IC(50)= 181 nM) of human IMR-90 lung fibroblasts expressing LPA(1) receptors. AM966 demonstrated a good pharmacokinetic profile following oral dosing in mice. In the mouse, AM966 reduced lung injury, vascular leakage, inflammation and fibrosis at multiple time points following intratracheal bleomycin instillation. AM966 also decreased lactate dehydrogenase activity and tissue inhibitor of metalloproteinase-1, transforming growth factor beta1, hyaluronan and matrix metalloproteinase-7, in bronchoalveolar lavage fluid. Anti-inflammatory agents.

别名 4'-(4-((((1R)-1-(2-氯苯基)乙氧基)羰基)氨基)-3-甲基-5-异恶唑基)-联苯-4-乙酸;;AM 966;AM-966; 4'-(4-((((1r)-1-(2-chlorophenyl)ethoxy)carbonyl)amino)-3-methyl-5-isoxazolyl)-(1,1'-biphenyl)-4-acetic acid;

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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途