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 有潜力用于特发性肺纤维化 (IPF) 的研究。

BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 ( LPA1 ) antagonist [1]. BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC 50 s of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respectively [2]. BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF) [3].

BMS-986020 sodium (0.1-10 nM; pre-incubated) concentration-dependent displacement of [ 18 F]BMT-083133 binding is observed in LPA1 + cells and lung sections. At 0.1 nM, the percent displacement in healthy mice, bleomycin mice, and IPF lungs is 18%, 24%, and 31%, respectively. At 10 nM, the percent displacement is 73%, 76%, and 64%, respectively.[ 18 F]BMT-083133, a radioligand targeting LPA1 is developed as a translational research tool for assessment of lung LPA1 engagement of BMS-986020 using in vitro autoradiography (ARG) [4].

1380650-53-2

C29H25N2NaO5

504.51

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years