1228690-19-4AM966

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商品编号：A125594

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商品名称：1228690-19-4AM966
商品毛重：0.00
单位：件
上架时间：2017-10-31 22:40:38

名称: AM966英文名称: AM966≥98%产品编号 A125594
CAS号: 1228690-19-4分子式 C₂₇H₂₃ClN₂O₅分子量490.93

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。
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;
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.