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S82913

AM095

源叶(MedMol) ≥98%
  • 英文名:
  • AM095
  • 别名:
  • 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;
  • CAS号:
  • 1345614-59-6
  • 分子式:
  • C27H23N2NaO5
  • 分子量:
  • 478.47
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S82913-5mg ≥98% ¥670.00元 10 - - - EA 加入购物车
源叶(MedMol) S82913-25mg ≥98% ¥2470.00元 10 - - - EA 加入购物车
源叶(MedMol) S82913-100mg ≥98% ¥6179.00元 10 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 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
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