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• 產(chǎn)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.

• 靶點(diǎn)： IC50: 0.98 μM (human LPA1), 0.73 μM (mouse LPA1);LPAReceptor;?LPLReceptor

• 體外研究：
  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)

• 體內(nèi)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

• 參考文獻(xiàn)：
  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

• 保存條件： -20°C

• 配置溶液濃度參考：
  

  	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

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *