BMS-986020

• Description:

  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].

• Product Name Alternative:

  AM152

• UNSPSC:

  12352005

• Hazard Statement:

  H315, H319, H335

• Target:

  LPL Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein

• Applications:

  COVID-19-immunoregulation

• Field of Research:

  Metabolic Disease; Inflammation/Immunology

• Assay Protocol:

  https://www.medchemexpress.com/BMS-986020.html

• Purity:

  99.91

• Solubility:

  DMSO : 125 mg/mL (ultrasonic)

• 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

• Molecular Formula:

  C29H26N2O5

• Molecular Weight:

  482.53

• Precautions:

  H315, H319, H335

• References & Citations:

  [1]Kihara Y, et al. Lysophospholipid receptors in drug discovery. Exp Cell Res. 2015 May 1;333 (2) :171-7.|[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.|[4]Adrienne Pena, et al. Autoradiographic evaluation of [18F]BMT-083133, a lysophosphatidic acid receptor 1 (LPA1) radioligand. The jornal of nuclear medicine.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 2

• CAS Number:

  1257213-50-5