1257213-50-5
Chemical Structure
BMS-986020
Synonym(s): AM152
- CAS No.: 1257213-50-5
- Formula:C29H26N2O5
- Molecular Weight:482.53
IUPAC Name: (R)-1-(4'-(3-methyl-4-(((1-phenylethoxy)carbonyl)amino)isoxazol-5-yl)-[1,1'-biphenyl]-4-yl)cyclopropane-1-carboxylic acid
InChIKey: GQBRZBHEPUQRPL-LJQANCHMSA-N
SMILES: O=C(C1(C2=CC=C(C3=CC=C(C4=C(NC(O[C@@H](C5=CC=CC=C5)C)=O)C(C)=NO4)C=C3)C=C2)CC1)O
Biological Activity: BMS-986020 (AM152) is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist[1]. BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respectively[2]. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF)[3].
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BMS-986020 | 99.83% | BMS-986020 (AM152) is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF). | ||||||||||||||||||||
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BMS-986020 (Standard) | ≥98% | BMS-986020 (Standard) is the analytical standard of BMS-986020 (HY-100619). This product is intended for research and analytical applications. BMS-986020 (AM152) is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF). | ||||||||||||||||||||
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References
- [1]. Kihara Y, et al. Lysophospholipid receptors in drug discovery. Exp Cell Res. 2015 May 1;333(2):171-7. [Content Brief]
- [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-Controlled, Phase 2 Trial of BMS-986020, a Lysophosphatidic Acid Receptor Antagonist for the Treatment of Idiopathic Pulmonary Fibrosis. Chest. 2018 Nov;154(5):1061-1069. [Content Brief]
