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)
In Vitro
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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.