BMS-986020 sodium

SKU: orb1686604

Description

BMS-986020 sodium is a potent and selective LPA1 receptor antagonist used in research on idiopathic pulmonary fibrosis (IPF), where it has been shown to slow FVC decline in clinical studies. Its off-target inhibition of hepatic transporters like BSEP also makes it a relevant tool for investigating drug-induced liver injury and bile acid homeostasis in vitro.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1380650-53-2
• MW: 504.51
• Purity: 99.83% (May vary between batches)
• Formula: C₂₉H₂₅N₂NaO₅
• SMILES: [O-]C(C1(C2=CC=C(C3=CC=C(C4=C(C(C)=NO4)NC(O[C@@H](C5=CC=CC=C5)C)=O)C=C3)C=C2)CC1)=O.[Na+]
• Target: LPL Receptor,LPA Receptor
• Solubility: DMSO:120 mg/mL (237.85 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:5 mg/mL (9.91 mM)

Bioactivity

• Target IC50:
  MDR3:7.5 μM|MRP4:6.2 μM|BSEP:4.8 μM
• In Vivo:
  BMS-986020 sodium (0.5, 2, 5, and 10 mg/kg, administered via gavage immediately or 3 hours after reperfusion) significantly reduced the cerebral infarction volume and neurological deficit scores induced by transient middle cerebral artery occlusion (tMCAO) in mice, with the most pronounced effects observed at doses of 5 and 10 mg/kg. Moreover, administration 3 hours after reperfusion provided equivalent protective efficacy.
• In Vitro:
  BMS-986020 sodium can inhibit the efflux transporters of bile acids in the liver, including BSEP (half-maximal inhibitory concentration IC₅₀ of 1.8μM), MRP3 (IC₅₀ of 22μM), and MRP4 (IC₅₀ of 6.2μM). At a concentration of 10μM, it suppresses the canalicular efflux of bile acids in Homo sapiens hepatocytes (inhibition rate of 68%). When the concentration reaches ≥10μM, BMS-986020 sodium impairs mitochondrial function in both Homo sapiens hepatocytes and cholangiocytes, including basal respiration, maximal respiration, adenosine triphosphate (ATP) production, and reserve capacity. Additionally, it inhibits phospholipid efflux in Homo sapiens hepatocytes (IC₅₀ for MDR3 is 7.5μM).

Storage & Handling

• Storage: keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BMS986020 sodium, AM152 sodium, AM-152 sodium

Compound Identifiers

PubChem CID

132274336