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CAS No. : 1380650-53-2
MCE 国际站:BMS-986020 sodium
产品活性: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。
研究领域:GPCR/G Protein
作用靶点:LPL Receptor
In Vitro: BMS-986020 sodium (0.1-10 nM; pre-incubated) concentration-dependent displacement of [18F]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.[18F]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).
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