819048-44-7
Chemical Structure
LY2112688
Synonym(s): Ac-(d-Arg)-CEH-(d-Phe)-RWC-NH2
- CAS No.: 819048-44-7
- Formula:C51H70N18O11S2
- Molecular Weight:1175.35
InChIKey: UNXFCHHFXJFRRB-ZSTGMXRXSA-N
SMILES: O=C([C@@H](NC([C@H](NC([C@@H](NC([C@@H](NC([C@H](CSSC[C@H](NC1=O)C(N)=O)NC([C@H](NC(C)=O)CCCNC(N)=N)=O)=O)CCC(O)=O)=O)CC2=CN=CN2)=O)CC3=CC=CC=C3)=O)CCCNC(N)=N)N[C@H]1CC4=CNC5=CC=CC=C45
Biological Activity: LY2112688 (Ac-(d-Arg)-CEH-(d-Phe)-RWC-NH2) is a synthetic peptide selective melanocortin 4 receptor (MC4R) agonist with a Ki of 0.13 nM for human MC4R and Ki values of 165, 74, and 1713 nM for human MC1R, MC3R, and MC5R, respectively. LY2112688 activates MC4R-mediated cAMP signaling and promotes PYY and GLP-1 release by activating peripheral MC4R in enteroendocrine L cells; Kir7.1 signaling in MC4R neurons is involved in its sustained suppression of food intake. LY2112688 inhibits food intake in vivo and can elevate heart rate and blood pressure. LY2112688 is useful for research on obesity, energy homeostasis, and MC4R signaling[1][2][3][4][5][6][7].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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LY2112688 | 99.96% | LY2112688 (Ac-(d-Arg)-CEH-(d-Phe)-RWC-NH2) is a synthetic peptide selective melanocortin 4 receptor (MC4R) agonist with a Ki of 0.13 nM for human MC4R and Ki values of 165, 74, and 1713 nM for human MC1R, MC3R, and MC5R, respectively. LY2112688 activates MC4R-mediated cAMP signaling and promotes PYY and GLP-1 release by activating peripheral MC4R in enteroendocrine L cells; Kir7.1 signaling in MC4R neurons is involved in its sustained suppression of food intake. LY2112688 inhibits food intake in vivo and can elevate heart rate and blood pressure. LY2112688 is useful for research on obesity, energy homeostasis, and MC4R signaling. | ||||||||||||||||||||
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References
- [1]. Kievit P, et al. Chronic treatment with a melanocortin-4 receptor agonist causes weight loss, reduces insulin resistance, and improves cardiovascular function in diet-induced obese rhesus macaques. Diabetes. 2013 Feb;62(2):490-7. [Content Brief]
- [2]. Møller CL, et al. Melanocortin agonists stimulate lipolysis in human adipose tissue explants but not in adipocytes. BMC research notes. 2015 Oct 12;8:559.
- [3]. Anderson EJP, et al. Late onset obesity in mice with targeted deletion of potassium inward rectifier Kir7.1 from cells expressing the melanocortin-4 receptor. Journal of neuroendocrinology. 2019 Jan;31(1):e12670.
- [4]. Panaro BL, et al. The melanocortin-4 receptor is expressed in enteroendocrine L cells and regulates the release of peptide YY and glucagon-like peptide 1 in vivo. Cell metabolism. 2014 Dec 02;20(6):1018-29.
- [5]. Greenfield JR, et al. Modulation of blood pressure by central melanocortinergic pathways. The New England journal of medicine. 2009 Jan 01;360(1):44-52.
- [6]. Molden BM, et al. Temporal cAMP Signaling Selectivity by Natural and Synthetic MC4R Agonists. Molecular endocrinology (Baltimore, Md.). 2015 Nov;29(11):1619-33.
- [7]. Møller CL, et al. Characterization of murine melanocortin receptors mediating adipocyte lipolysis and examination of signalling pathways involved. Molecular and cellular endocrinology. 2011 Jul 20;341(1-2):9-17.
