BMS-986020 sodium 是高亲和力溶血磷脂酸受体 1 (LPA1) 拮抗剂。BMS-986020 sodium 抑制胆汁酸和磷脂转运蛋白，抑制 BSEP，MRP4 和 MDR3，IC50 值分别为 4.8 μM，6.2 μM 和 7.5 μM。BMS-986020 sodium 用于治疗特发性肺纤维化 (IPF)。
货号:ajcx14832
CAS:1380650-53-2
分子式:C29H25N2NaO5
分子量：504.51
溶解度:DMSO: 150 mg/mL (297.32 mM); H2O:< 0.1 mg/mL (insoluble)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist[1].BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively[2]. BMS-986020 sodium is used for the treatment of idiopathic pulmonary fibrosis (IPF)[3].

[1]. Kihara Y, et al. Lysophospholipid receptors in drug discovery. Exp Cell Res. 2015 May 1;333(2):171-7. [2]. Glenn Rosen, et al. LPA1 antagonists BMS-986020 and BMS-986234 for idiopathic pulmonary fibrosis: Preclinical evaluation of hepatobiliary homeostasis. European Respiratory Journal. [3]. Palmer SM, et al. Randomized, Double-Blind, Placebo-Controlled, Phase 2 Trial of BMS-986020, a Lysophosphatidic Acid Receptor Antagonist for the Treatment of Idiopathic Pulmonary Fibrosis. Chest. 2018 Nov;154(5):1061-1069.