Ac-(D-Arg)-CEH-(D-Phe)-RWC-NH2 (trifluoroacetate salt)

Ac-(D-Arg)-CEH-(D-Phe)-RWC-NH₂ is a cyclic peptide and an agonist of melanocortin receptor 4 (MC4R).¹ It induces cAMP release in HEK293 cells expressing human MC4R (EC₅₀ = 0.28 nM). Ac-(D-Arg)-CEH-(D-Phe)-RWC-NH₂ is selective for MC4R over MC1R, MC3R, and MC5R (K_is = 0.55, 16.78, 56.79, and >500 nM, respectively). It decreases food intake and body weight in a rat model of diet-induced obesity when administered at doses of 0.075 or 0.299 ?mol/kg.

References:
[1]. Mayer, J.P., Hsiung, H.M., Flora, D.B., et al.Discovery of a β-MSH-derived MC-4R selective agonistJ. Med. Chem.48(9)3095-3098(2005).