S82913 |
AM095 |
源叶(MedMol) | ≥98% |
- 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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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)