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. Form:Solid IC50& Target:IC50: 4.8 µM (BSEP),6.2 µM (MRP4),7.5 µM (MDR3)
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BMS-986020 sodium
CAS number:1380650-53-2 molecular formula:C29H25N2NaO5
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1380650-53-2 | molecular formula | C29H25N2NaO5 |
| molecular weight | 504.51 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
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