BMS-986020

Catalog No.S3572 Batch:S357202

Technical Data

Formula	C₂₉H₂₆N₂O₅
Molecular Weight	482.53	CAS No.	1257213-50-5
Solubility (25°C)*	In vitro	DMSO	97 mg/mL (201.02 mM)
		Ethanol	12 mg/mL (24.86 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]

Protocol (from reference)

Cell Assay:^{^[2]}	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.

Cell Assay:^{^[2]}

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.

References

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SHIPPING AND STORAGE
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