| Identification | Back Directory | [Name]
AC-D-ARG-CYS-GLU-HIS-D-PHE-ARG-TRP-CYS-NH2 | [CAS]
819048-44-7 | [Synonyms]
Reaxys ID: 14573809
AC-D-ARG-CYS-GLU-HIS-D-PHE-ARG-TRP-CYS-NH2
52:PN:WO2005000339 SEQID:52 claimed sequence
Acetyl-(D-Arg10,Cys11,D-Phe14,Cys17)-β-MSH (10-17) amide
Acetyl-(D-Arg10,Cys11,D-Phe14,Cys17)-b-MSH (10-17) aMide
AC-D-ARG-CYS-GLU-HIS-D-PHE-ARG-TRP-CYS-NH2, (DISULFIDE BOND)
ACETYL-(D-ARG10, CYS11, D-PHE14, CYS17)-BETA-MSH (10-17) AMIDE
Ac-D-Arg-Cys-Glu-His-D-Phe-Arg-Trp-Cys-NH2(Disulfide bridge：Cys2-Cys8)
Acetyl-(D-Arg10,Cys11,D-Phe14,Cys17)-b-MSH (10-17) amide trifluoroacetate salt | [Molecular Formula]
C51H72N18O11S2 | [MDL Number]
MFCD08458545 | [MOL File]
819048-44-7.mol | [Molecular Weight]
1177.36 |
| Chemical Properties | Back Directory | [density ]
1.56±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [form ]
lyophilized powder | [pka]
4.47±0.10(Predicted) | [color ]
white to off-white | [Sequence]
Ac-{d-Arg}-Cys-Glu-His-{d-Phe}-Arg-Trp-Cys-NH2 (Disulfide bridge: Cys2-Cys8) |
| Hazard Information | Back Directory | [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-affinitypotent and selective melanocortin receptor 4 (MC-4MC-4RMC4-RMC4R) 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 nMMC-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 |
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