BMS-986020 (AM152) 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 (AM152) sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. 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. BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).

Solid

IC50: 4.8 μM (BSEP); 6.2 μM (MRP4); 7.5 μM (MDR3)

BMS-986020 sodium (0.1-10 nM; pre-incubated) concentration-dependent displacement of [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.
[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). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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-Controlle

In Vitro: DMSO : 150 mg/mL (297.32 mM; Need ultrasonic)配制储备液