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BMS-986020

    
≥99%

BMS-986020

源叶(MedMol)
S82609 一键复制产品信息
1257213-50-5
C29H26N2O5
482.5271
1-{4'-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-biphenyl-4-yl}-cyclopropanecarboxylic acid; (R)-1-(4'-(3-methyl-4-((1-phenylethoxy)carbonylamino)isoxazol-5-yl)biphenyl-4-yl)cyclopr
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
S82609-5mg
≥99%

¥330.00

10 - - - -
S82609-10mg
≥99%

¥594.00

9 - - - -
S82609-25mg
≥99%

¥1260.00

5 - - - -
S82609-50mg
≥99%

¥2140.00

5 - - - -
S82609-100mg
≥99%

¥3640.00

3 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
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: 部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。

参考文献

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