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S82467

AM095 (free acid)

源叶(MedMol) ≥98%
  • 英文名:
  • AM095 (free acid)
  • 别名:
  • [4'-[3-甲基-4-[[[((R)-1-苯基乙基)氧基]羰基]氨基]异恶唑-5-基]联苯-4-基]乙酸;(R)-2-(4'-(3-methyl-4-((1-phenylethoxy)carbonylamino)isoxazol-5-yl)biphenyl-4-yl)acetic acid; CS-1129; AM095; AM-095 free base; AM095 (free acid);
  • CAS号:
  • 1228690-36-5
  • 分子式:
  • C27H24N2O5
  • 分子量:
  • 456.4899
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) S82467-5mg ≥98% ¥132.00元 6 - - - EA 加入购物车
源叶(MedMol) S82467-10mg ≥98% ¥235.00元 6 - - - EA 加入购物车
源叶(MedMol) S82467-25mg ≥98% ¥451.00元 4 - - - EA 加入购物车
源叶(MedMol) S82467-50mg ≥98% ¥797.00元 3 - - - EA 加入购物车
源叶(MedMol) S82467-100mg ≥98% ¥1331.00元 1 - - - 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 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.
  • 靶点: IC50: 0.98 μM (human LPA1), 0.73 μM (mouse LPA1);LPAReceptor; LPLReceptor
  • 体外研究:
    AM095 inhibits the LPA-induced calcium flux of CHO cells stably transfected with human or mouse LPA1. 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. AM095 reduces LPA-induced vasorelaxation by appr 90% at 10 μM as compared to vehicle control. AM095 inhibits LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM)
  • 体内研究:
    Pharmacological antagonism of LPA1 with AM095 significantly attenuates bleomycin-induced dermal fibrosis. 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. AM095 dose-dependently reduces LPA-stimulated histamine release. AM095 attenuates bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid. AM095 decreases kidney fibrosis in a mouse unilateral ureteral obstruction model
  • 参考文献:
    1. 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 2. Ruisanchez E, et al. Lysophosphatidic acid induces vasodilation mediated by LPA1 receptors, phospholipase C, and endothelial nitric oxide synthase. FASEB J. 2014 Feb;28(2):880-90 3. Swaney, J. S., et al. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. Journal of Pharmacology and Experimental Therapeutics (2011), 336(3), 693-700.
  • 溶解性: soluble  in  DMSO
  • 保存条件: -20°C
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.191 ml 10.953 ml 21.906 ml
    5 mM 0.438 ml 2.191 ml 4.381 ml
    10 mM 0.219 ml 1.095 ml 2.191 ml
    50 mM 0.044 ml 0.219 ml 0.438 ml
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