BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 sodium 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 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).

Product information

CAS Number: 1380650-53-2

Molecular Weight: 504.51

Formula: C29H25N2NaO5

Chemical Name: sodium 1-{4'-[3-methyl-4-({[(1R)-1-phenylethoxy]carbonyl}amino)-1,2-oxazol-5-yl]-[1,1'-biphenyl]-4-yl}cyclopropane-1-carboxylate

Smiles: [Na+].CC1=NOC(=C1NC(=O)O[C@H](C)C1C=CC=CC=1)C1C=CC(=CC=1)C1C=CC(=CC=1)C1(CC1)C([O-])=O

InChiKey: QDCOVTLBRMPIMY-FSRHSHDFSA-M

InChi: InChI=1S/C29H26N2O5.Na/c1-18-25(30-28(34)35-19(2)20-6-4-3-5-7-20)26(36-31-18)23-10-8-21(9-11-23)22-12-14-24(15-13-22)29(16-17-29)27(32)33;/h3-15,19H,16-17H2,1-2H3,(H,30,34)(H,32,33);/q;+1/p-1/t19-;/m1./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 150 mg/mL (297.32 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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).

Products are for research use only. Not for human use.