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AM095, LPA1 受体拮抗剂

    
≥98%

AM095

源叶(MedMol)
S82913 一键复制产品信息
1345614-59-6
C27H23N2NaO5
478.47
4'-[3-甲基-4-[[[(1R)-1-苯基乙氧基]羰基]氨基]-5-异恶唑基]联苯-4-乙酸钠盐;AM095||AM-095; CS-1118; sodium (4'-(3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl)-biphenyl-4-yl)-acetic acid; AM-095;;AM095
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
S82913-5mg
≥98%

¥676.00

10 3 - - -
S82913-25mg
≥98%

¥2220.00

10 - - - -
S82913-100mg
≥98%

¥5560.00

8 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.
靶点: LPA1 receptor;LPAReceptor; LPLReceptor
体内研究: AM095 has high oral bioavailability and a moderate half-life and is well tolerated at the doses tested in rats and dogs after oral and intravenous dosing. After oral (10 mg/kg) dosing in rats, AM095 plasma concentrations peaked at 2 h with a Cmax of 41 μM, thereafter decreasing to 10 nM by 24 h. After intravenous (2 mg/kg) dosing, a Cmax of 12 μM is observed within 15 min, which also decreased to approximately 10 nM by 24 h, yielding a t1/2 of 1.79 h. In dogs, a single oral dose of 5 mg/kg yielded a peak plasma concentration of 21 μM within 15 min of dosing, which then decreased to 10 nM by 24 h. In contrast, an intravenous dose of 2 mg/kg resulted in a Cmax of 11 μM within 15 min and decreased to 15 nM by 8 h, yielding a t1/2 of 1.5 h
参考文献: 1. Swaney JS, et al. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. J Pharmacol Exp Ther. 2011 Mar;336(3):693-700. 2. Castelino FV, et al. Amelioration of dermal fibrosis by genetic deletion or pharmacologic antagonism of lysophosphatidic acid receptor 1 in a mouse model of scleroderma. Arthritis Rheum. 2011 May;63(5):1405-15.
溶解性: Soluble  in  DMSO
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.09 ml 10.45 ml 20.9 ml
5 mM 0.418 ml 2.09 ml 4.18 ml
10 mM 0.209 ml 1.045 ml 2.09 ml
50 mM 0.042 ml 0.209 ml 0.418 ml
注意: 部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。

参考文献

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