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• 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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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