BMS-470539

• UNSPSC Description:

  BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation[1].

• Target Antigen:

  Melanocortin Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein;Neuronal Signaling

• Applications:

  Cancer-programmed cell death

• Field of Research:

  cancer

• Assay Protocol:

  https://www.medchemexpress.com/bms-470539.html

• Solubility:

  10 mM in H2O

• Smiles:

  CCCC(C1(C2=CC=CC=C2)CCN(C([C@@H](CC3=CC=C(C=C3)OC)NC([C@H](CC4=CN=CN4C)N)=O)=O)CC1)=O

• Molecular Weight:

  559.70

• References & Citations:

  [1]A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported

• CAS Number:

  457893-92-4