For research use only. Not for therapeutic Use.
BMS-470539 dihydrochloride(CAT: I046017) is a highly potent and selective melanocortin-1 receptor (MC1R) agonist, with IC₅₀ and EC₅₀ values of 120 nM and 28 nM, respectively. It shows no activity at MC3R and functions only as a weak partial agonist at MC4R and MC5R. BMS-470539 exhibits strong anti-inflammatory activity by reducing TNF-α–stimulated NF-κB luciferase activity and inhibiting NF-κB nuclear translocation in melanoma cells. In vivo, it suppresses leukocyte adhesion and emigration, while reducing CXCL1 and CCL2 expression without affecting cell rolling. This selective MC1R agonist is a valuable tool for investigating melanocortin signaling, inflammation, and immune-mediated disease mechanisms.
| CAS Number | 2341796-82-3 |
| Synonyms | (2S)-2-amino-N-[(2R)-1-(4-butanoyl-4-phenylpiperidin-1-yl)-3-(4-methoxyphenyl)-1-oxopropan-2-yl]-3-(3-methylimidazol-4-yl)propanamide;dihydrochloride |
| Molecular Formula | C32H43Cl2N5O4 |
| Purity | ≥95% |
| IUPAC Name | (2S)-2-amino-N-[(2R)-1-(4-butanoyl-4-phenylpiperidin-1-yl)-3-(4-methoxyphenyl)-1-oxopropan-2-yl]-3-(3-methylimidazol-4-yl)propanamide;dihydrochloride |
| InChI | InChI=1S/C32H41N5O4.2ClH/c1-4-8-29(38)32(24-9-6-5-7-10-24)15-17-37(18-16-32)31(40)28(19-23-11-13-26(41-3)14-12-23)35-30(39)27(33)20-25-21-34-22-36(25)2;;/h5-7,9-14,21-22,27-28H,4,8,15-20,33H2,1-3H3,(H,35,39);2*1H/t27-,28+;;/m0../s1 |
| InChIKey | DUAOBJHRUKFKIH-YDVFRNEYSA-N |
| SMILES | CCCC(=O)C1(CCN(CC1)C(=O)C(CC2=CC=C(C=C2)OC)NC(=O)C(CC3=CN=CN3C)N)C4=CC=CC=C4.Cl.Cl |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
