| 产品描述: | BMS-986020 (AM152, AP-3152 free acid) 是一种有效的 lysophosphatidic acid receptor 1 (LPA1) 的选择性拮抗剂。BMS-986020 可抑制胆汁酸和磷脂转运蛋白,对于BSEP、MRP4和MDR3的IC50值分别为4.8 μM、6.2 μM和7.5 μM。BMS-986020 具有治疗特发性肺纤维化 idiopathic pulmonary fibrosis (IPF) 的潜力 |
| 靶点: |
LPA1; BSEP(Cell-free assay): 4.8 μM; MRP4(Cell-free assay):6.2 μM; MDR3(Cell-free assay):7.5 μM;LPAReceptor; LPLReceptor |
| 体外研究: |
BMS-986020, a selective and potent lysophosphatidic acid receptor 1 (LPA1) inhibitor, inhibits LPA1-induced fibrogenesis in the Scar-in-a-Jar in vitro model |
| 细胞实验: |
Cell lines: Human lung fibroblasts Concentrations: 12 days Incubation Time: 0.01, 0.05, 0.1, 0.5, 1, or 5 µM Method: Human lung fibroblasts were cultured in 48-well plates in Dulbecco’s Modified Eagle Medium (DMEM) + GlutaMax with 0.4% fetal bovine serum, 37.5 mg/mL Ficoll 70, 25 mg/mL Ficoll 400, and 1% ascorbic acid. Cells were stimulated with 1 ng/mL transforming growth factor beta 1 (TGF-β1) or 20 µM LPA with or without BMS-986020 (0.01, 0.05, 0.1, 0.5, 1, or 5 µM) diluted in dimethyl sulfoxide (DMSO), or vehicle (0.05% DMSO) in four replicates. Cells were cultured at 37 °C with 95% O2 and 5% CO2 for 12 days, and medium was changed at Day 4 and 8. Supernatants were stored at − 20 °C until biomarker measurements. alamarBlue was used to quantify cellular metabolism at Day 0 (prior to drug treatment) and Day 12. Release of lactate dehydrogenase (LDH) was quantified at Day 4, 8, and 12. |
| 参考文献: |
1. Glenn Rosen, et al. LPA1 antagonists BMS-986020 and BMS-986234 for idiopathic pulmonary fibrosis: Preclinical evaluation of hepatobiliary homeostasis. European Respiratory Journal 2017 50: PA1038; vol. 50 no. suppl 61. 2. Decato BE, et al. LPA1 antagonist BMS-986020 changes collagen dynamics and exerts antifibrotic effects in vitro and in patients with idiopathic pulmonary fibrosis. Respir Res. 2022 Mar 18;23(1):61. |
| 溶解性: |
Soluble in DMSO、Ethanol |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.072 ml |
10.362 ml |
20.724 ml |
| 5 mM |
0.414 ml |
2.072 ml |
4.145 ml |
| 10 mM |
0.207 ml |
1.036 ml |
2.072 ml |
| 50 mM |
0.041 ml |
0.207 ml |
0.414 ml |
|
| 注意: |
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