S82467 |
AM095 (free acid) |
| 源叶(MedMol) | 98% |
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- 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)
- 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℃
- 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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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
