Home GPCR & G Protein LPA Receptor antagonist BMS-986020 For research use only.

BMS-986020

Synonyms: AM152, AP-3152 free acid

BMS-986020 (AM152, AP-3152 free acid) is a potent and selective antagonist of lysophosphatidic acid receptor 1 (LPA1). BMS-986020 inhibits bile acid and phospholipid transporters with IC50 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).

BMS-986020 Chemical Structure

BMS-986020 Chemical Structure

CAS No. 1257213-50-5

Purity & Quality Control

BMS-986020 Related Products

Signaling Pathway

LPA Receptor Signaling Pathways

LPA Receptor Signaling Pathway

Biological Activity

Description BMS-986020 (AM152, AP-3152 free acid) is a potent and selective antagonist of lysophosphatidic acid receptor 1 (LPA1). BMS-986020 inhibits bile acid and phospholipid transporters with IC50 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).
Targets
LPA1 [1] BSEP [1]
(Cell-free assay)		 MRP4 [1]
(Cell-free assay)		 MDR3 [1]
(Cell-free assay)
4.8 μM 6.2 μM 7.5 μM
In vitro
In vitro

BMS-986020, a selective and potent lysophosphatidic acid receptor 1 (LPA1) inhibitor, inhibits LPA1-induced fibrogenesis in the Scar-in-a-Jar in vitro model[2]
Cell Research Cell lines Human lung fibroblasts
Concentrations 12 days
Incubation Time 0.01, 0.05, 0.1, 0.5, 1, or 5 µM
Method

Human lung fibroblasts were cultured in 48-well plates in Dulbecco’s Modified Eagle Medium (DMEM) + GlutaMax with 0.4% fetal bovine serum, 37.5 mg/mL Ficoll 70, 25 mg/mL Ficoll 400, and 1% ascorbic acid. Cells were stimulated with 1 ng/mL transforming growth factor beta 1 (TGF-β1) or 20 µM LPA with or without BMS-986020 (0.01, 0.05, 0.1, 0.5, 1, or 5 µM) diluted in dimethyl sulfoxide (DMSO), or vehicle (0.05% DMSO) in four replicates. Cells were cultured at 37 °C with 95% O2 and 5% CO2 for 12 days, and medium was changed at Day 4 and 8. Supernatants were stored at  − 20 °C until biomarker measurements. alamarBlue was used to quantify cellular metabolism at Day 0 (prior to drug treatment) and Day 12. Release of lactate dehydrogenase (LDH) was quantified at Day 4, 8, and 12.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02101125 Completed
Immunosuppression For Disease
Bristol-Myers Squibb
 March 2014 Phase 1
NCT02068053 Completed
Immunosuppression For Disease
Bristol-Myers Squibb
 March 2014 Phase 1
NCT02017730 Completed
Immunology
Bristol-Myers Squibb
 January 2014 Phase 1
NCT01766817 Completed
Idiopathic Pulmonary Fibrosis
Bristol-Myers Squibb
 January 31 2013 Phase 2

Chemical Information & Solubility

Molecular Weight 482.53 Formula

C29H26N2O5
CAS No. 1257213-50-5 SDF --
Smiles CC(OC(=O)NC1=C(ON=C1C)C2=CC=C(C=C2)C3=CC=C(C=C3)C4(CC4)C(O)=O)C5=CC=CC=C5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 97 mg/mL ( (201.02 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 97 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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