BMS-470539 dihydrochloride

SKU: orb1710237

Description

BMS-470539 dihydrochloride is a potent and selective MC1R agonist with demonstrated anti-inflammatory properties. Research indicates it mitigates oxidative stress and neuronal apoptosis via the MC1R/cAMP/PKA/Nurr1 pathway, showing protective effects in neonatal hypoxia-ischemia models, supporting its use in neuroinflammation and neuroprotection studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2341796-82-3
• MW: 632.62
• Purity: >99.99% (May vary between batches)
• Formula: C₃₂H₄₃Cl₂N₅O₄
• SMILES: CCCC(C1(C2=CC=CC=C2)CCN(CC1)C([C@H](NC([C@@H](N)CC3=CN=CN3C)=O)CC4=CC=C(C=C4)OC)=O)=O.Cl.Cl
• Target: Melanocortin Receptor

Bioactivity

• Target IC50:
  MC1R:120 nM|MC1R:28 nM (EC50)
• In Vivo:
  METHODS: BMS-470539 dihydrochloride (2.05-18.47 mg/kg, intravenous injection, 125 minutes) was used to treat WT and MC1 receptor-negative e/e mice to study its effects on mesenteric microcirculation. RESULTS:BMS-470539 dihydrochloride treatment of mice inhibited cell adhesion and migration, had no effect on cell rolling, and also inhibited the tissue expression of two chemokines, CXCL1 and CCL2.
• In Vitro:
  METHODS: BMS-470539 dihydrochloride (0-1μM, 15 minutes) was used to treat HBL cells stably transfected with NF-B luciferase reporter gene, and then treated with 0.5 ng/mL TNF-α for 4 hours to study its effect on stable transfection. Effects of NF-B luciferase reporter gene on TNF-α-stimulated luciferase activation in HBL cells. RESULTS:BMS-470539 dihydrochloride treatment of HBL cells with NF-B luciferase reporter gene caused a dose-dependent significant reduction in TNF-α-stimulated NF-B luciferase activity.

Storage & Handling

• Storage: store at low temperature,keep away from moisture | 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

BMS470539, BMS-470539, BMS470539 dihydrochloride, BMS-470539 Dihydrochloride, BMS 470539, BMS 470539 dihydrochloride, Melanocortin Receptor, Melanocortin-1 receptor, MelanocortinReceptor

Compound Identifiers

PubChem CID

60210130