Ac-D-Arg-Cys-Glu-His-D-Phe-Arg-Trp-Cys-NH2

Uses

Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH 2 is a cyclic octapeptide with MC4R agonism. Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH 2 significantly increases heart rate and blood pressure[1].

Biological Activity

LY2112688 is a beta-melanocyte-stimulating hormone (β-MSH)-derived peptide th at acts as a high-affinity, potent and selective melanocortin receptor 4 (MC-4, MC-4R, MC4-R, MC4R) agonist (human/r at MC-4 Ki = 0.55/0.39 nM; human MC-1/3/5 Ki = 16.78/56.79/>500 nM). LY2112688 selectively induces MC-4-mediated cAMP release (MC-4/3 EC50 = 0.25 nM/1.61 nM, MC-4/3 Emax = 94.5%/84.1% of NDP-α-MSH Emax using HEK293 expressing respective human receptors) and exhibits in vivo efficacy in reducing daily food intake and promoting weight loss among diet-induced obese rats (75 & 299 nmol/kg/day s.c.).

References

[1] Doering SR, et al. Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign. J Med Chem. 2021 May 13;64(9):5577-5592. doi: 10.1021/acs.jmedchem.0c02041. Epub 2021 Apr 22. Erratum in: J Med Chem. 2023 May 25;66(10):7063-7065. DOI:10.1021/acs.jmedchem.0c02041