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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1228690-36-5
- 规格：
10 mM * 1 mL/500 mg/5 mg/10 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1050.0 |
|---|---|---|---|
| 规格： | 500 mg | 产品价格： | 询价 |
| 规格： | 5 mg | 产品价格： | ￥950.0 |
| 规格： | 10 mg | 产品价格： | ￥1500.0 |
| 规格： | 50 mg | 产品价格： | ￥4500.0 |
| 规格： | 100 mg | 产品价格： | ￥7000.0 |
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AM095 free acid
CAS No. : 1228690-36-5
MCE 国际站：AM095 free acid
产品活性：AM095 free acid 是一种有效的 LPA1 受体拮抗剂，对重组人和小鼠 LPA1 的 IC50 值分别为 0.98 和 0.73 μM。
研究领域：GPCR/G Protein
作用靶点：LPL Receptor
In Vitro: 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).
In Vivo: 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.
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