All Photos(1)
Synonym(s):
Ac-D-Arg-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH2, trifluoroacetate salt, Ac-D-Arg-cyclo[Cys-Glu-His-D-Phe-Arg-Trp-Cys]-NH2, trifluoroacetate salt, Ac-rCEHfRWC-NH2, TFA (D-amino acids in lower case; C2→C8 disulfide), Acetyl-D-Arg-Cys-Glu-His-D-Phe-Arg-Trp-Cys-NH2, trifluoroacetate salt (Cys2→Cys8 disulfide), LY 2112688 TFA salt, LY-2112688 TFA salt
Empirical Formula (Hill Notation):
C51H70N18O11S2 · xC2HF3O2
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Biochem/physiol Actions
LY2112688 is a beta-melanocyte-stimulating hormone (β-MSH)-derived peptide that acts as a high-affinity, potent and selective melanocortin receptor 4 (MC-4, MC-4R, MC4-R, MC4R) agonist (human/rat 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.).
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Paul Kievit et al.
Diabetes, 62(2), 490-497 (2012-10-11)
The melanocortin-4 receptor (MC4R) is well recognized as an important mediator of body weight homeostasis. Activation of MC4R causes dramatic weight loss in rodent models, and mutations in human are associated with obesity. This makes MC4R a logical target for
Karine Clément et al.
Nature medicine, 24(5), 551-555 (2018-05-08)
Genetic defects underlying the melanocortin-4 receptor (MC4R) signaling pathway lead to severe obesity. Three severely obese LEPR-deficient individuals were administered the MC4R agonist setmelanotide, resulting in substantial and durable reductions in hyperphagia and body weight over an observation period of
Jerry R Greenfield et al.
The New England journal of medicine, 360(1), 44-52 (2008-12-19)
Weight gain and weight loss are associated with changes in blood pressure through unknown mechanisms. Central melanocortinergic signaling is implicated in the control of energy balance and blood pressure in rodents, but there is no information regarding such an association
John P Mayer et al.
Journal of medicinal chemistry, 48(9), 3095-3098 (2005-04-29)
A series of novel, disulfide-constrained human beta-melanocyte stimulating hormone (beta-MSH)-derived peptides were optimized for in vitro melanocortin-4 receptor (MC-4R) binding affinity, agonist efficacy, and selectivity. The most promising of these, analogue 18, was further studied in vivo using chronic rat
Cathrine Laustrup Møller et al.
Molecular and cellular endocrinology, 341(1-2), 9-17 (2011-05-28)
The melanocortin receptors (MCRs) belong to the G-protein coupled receptors (family A). So far, 5 different subtypes have been described (MC1R-MC5R) and of these MC2R and MC5R have been proposed to act directly in adipocytes and regulate lipolysis in rodents.
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