NEW! Novel Melanocortin Pharmacology Peptide Now Available from Peptides International

Novel Melanocortin Pharmacology Peptide Now Available from Peptides International
Melanocortin receptors (MCR1-MCR5) belong to the G-protein coupled receptor (GPCRs) family whose endogenous ligands are derived by posttranslational cleavage of the pro-opiomelanocortin (POMC) gene. A common motif for these known agonists is the tetrapeptide sequence, His-Phe-Arg-Trp. Presently, there are only two known endogenous antagonists for the melanocortin receptor family, agouti and the agouti-related protein (AGRP). It has been reported that melanocortin-3 and -4 receptors (MC3R, MC4R) are involved in feeding behavior, obesity, metabolism, and energy homeostasis in knockout mice and also that melanocortin-1 receptor (MC1R) is involved in skin pigmentation and animal coat coloration.^1,2,3 Interestingly, Melanocortin-5 receptor (MC5R) is expressed in a variety of peripheral tissues and has been deleted from the mouse genome. MC5R is thought to be involved in exocrine gland function. Recently, University of Florida researchers reported that a novel ligand, Ac-His-D-Phe(p-Iodo)-Arg-Trp-NH₂,⁴is a full nanomolar agonist at the mMC1 and mMC5 receptors, mMC3R partial agonist with potent antagonist activity (pA₂ = 7.25, Ki = 56 nM), and a potent agonist at the mMC4R (EC₅₀ = 25 nM). This ligand was reported to possess novel melanocortin receptor pharmacology, as compared to previously reported peptides, and is thought to be useful for in vivo studies to differentiate MC3R vs MC4R physiological roles in animal models, such as primates, where “knockout” animals are not viable options.

CODE	PRODUCT	QTY	USD
PMC-3684-PI NEW!	Ac-His-D-Phe(p-Iodo)-Arg-Trp-NH₂Acetyl-L-Histidyl-p-Iodo-D-Phenylalanyl-L- Arginyl-L-Tryptophan Amide (M.W. 811.69) C₃₄H₄₂N₁₁O₅I Melanocortin Receptor 1/4/5 Agonist / Receptor 3 Antagonist • This product is sold under license granted by the University of Florida Research Foundation.	1 mg 5 mg	68 195

1. R.D. Cone, D. Lu, S. Kopula, D.I. Vage, H. Klungland, B. Boston, W. Chen, D.N. Orth, C. Pouton, R.A. Kesterson, Recent Prog. Horm. Res., 51, 287-318 (1996). 2. M.E. Hadley, V.J. Hruby, J. Jiang, S.D. Sharma, J.L. Fink, C. Haskell-Luevano, D.L. Bentley, F. al-Obeidi, and T.K. Sawyer, Pigment Cell Res., 9, 213-34 (1996). 3. D.J. MacNeil, A.D. Howard, X. Guan, T.M. Fong, R.P. Nargund, M.A. Bednarek, M.T. Goulet, D.H. Weinberg, A.M. Strack, D.J. Marsh, H.Y. Chen, C.-P. Shen, A.S. Chen, C.I. Rosenblum, T. MacNeil, M. Tota, E.D. MacIntyre, and L.H.T. Van der Ploeg, Eur. J. Pharmacol., 450, 93 (2002). 4. J.R. Holder, R.M. Bauzo, Z. Xiang, and C. Haskell-Luevano, J. Med. Chem., 45, 3073-3081 (2002).
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