BMS-986020 Chemical Properties

Melting point:

174-180°C

Boiling point:

664.8±55.0 °C(Predicted)

Density 

1.309±0.06 g/cm3(Predicted)

storage temp. 

-20°C Freezer

solubility 

DMSO (Slightly), Methanol (Slightly, Sonicated)

form 

Solid

pka

4.19±0.20(Predicted)

color 

White to Off-White

InChIKey

GQBRZBHEPUQRPL-LJQANCHMSA-N

SMILES

C1(C2=CC=C(C3=CC=C(C4ON=C(C)C=4NC(O[C@@H](C4=CC=CC=C4)C)=O)C=C3)C=C2)(C(O)=O)CC1

BMS-986020 Usage And Synthesis

Description

BMS 986020 is a potent G protein-coupled lysophosphatidic acid receptor 1 (LPA₁) antagonist with an IC₅₀ value less than 300 nM for human LPA₁ expressing CHO cells. Formulations containing BMS 986020 are being investigated in clinical trials for efficacy in idiopathic pulmonary fibrosis.

Uses

BMS-?986020 is an LPA-1 antagonist which may be used in the inhibition and treatment of bleomycin-induced pulminary fibrosis.

References

[1] PETER T. W. CHENG*. Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases[J]. Journal of Medicinal Chemistry, 2021, 64 21: 15549-15581. DOI: 10.1021/acs.jmedchem.1c01256
[2] VEERESA GUDUDURU . Identification of Darmstoff analogs as selective agonists and antagonists of lysophosphatidic acid receptors[J]. Bioorganic & Medicinal Chemistry Letters, 2006, 16 2: Pages 451-456. DOI: 10.1016/j.bmcl.2005.08.096
[3] L. SIVARAMAN . Structure dependence and species sensitivity of in vivo hepatobiliary toxicity with lysophosphatidic acid receptor 1 (LPA1) antagonists[J]. Toxicology and applied pharmacology, 2022, 438: Article 115846. DOI: 10.1016/j.taap.2021.115846
[4] BHAKTA PRASAD GAIRE  Ji W C  Arjun Sapkota. BMS-986020, a Specific LPA1 Antagonist, Provides Neuroprotection against Ischemic Stroke in Mice.[J]. Antioxidants, 2020, 9 11. DOI: 10.3390/antiox9111097

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