Product Name:HS 014
Synonyms:3-[[2-[[1-[1-[25-acetamido-13-(3-carbamimidamidopropyl)-22-(2-carboxyethyl)-19-(1H-imidazol-4-ylmethyl)-10-(1H-indol-3-ylmethyl)-16-(naphthalen-2-ylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carbonyl]pyrroli
CAS No:207678-81-7
Purity:95%
Molar Mass:1563.8
Chemical Formula:C71H94N20O17S2
Storage:Store at -20 degrees Celsius
Sequence:CEHXRWGCPPKD
Target:melanocortin-4 receptor
Application:
HS 014 is a selective melanocortin-4 receptor (MC4R) agonist, commonly used in research to study the role of MC4R in regulating energy homeostasis, appetite, and body weight. This peptide is particularly valuable in investigations related to obesity, metabolic disorders, and the central control of feeding behavior. HS 014 exhibits high specificity and affinity for MC4R, allowing researchers to precisely target and modulate this receptor??s activity in various experimental settings. With its high purity and stability, HS 014 provides reliable and reproducible results, making it an essential tool for studies in neuroendocrinology and metabolic research.
Current Research:
HS 014 (CAS: 207678-81-7) is a potent and selective antagonist of the melanocortin-4 receptor (MC4R), a G protein-coupled receptor implicated in the regulation of energy homeostasis, feeding behavior, and nociception. The peptide exhibits high affinity for human MC4R, with a Ki value of 3.16 nM, and demonstrates significantly lower affinities for other melanocortin receptor subtypes, including MC1R (Ki = 108 nM), MC3R (Ki = 54.4 nM), and MC5R (Ki = 694 nM), underscoring its selectivity.
Chemical Structure and Properties
HS 014 is a synthetic peptide with the sequence Ac-Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH₂, where D-2-Nal represents D-2-naphthylalanine. The peptide includes an N-terminal acetyl group and a C-terminal amide, with a disulfide bridge between the cysteine residues at positions 1 and 8, contributing to its conformational stability. It has a molecular weight of 1563.77 g/mol and is soluble in water up to 1 mg/mL.
Pharmacological Effects
In vivo studies have demonstrated that central administration of HS 014 increases food intake in free-feeding rats, indicating its role in modulating appetite through MC4R antagonism. Additionally, HS 014 has been shown to enhance nociceptive responses in mice, suggesting its involvement in pain perception pathways. The peptide also inhibits interleukin-1β-induced Fos expression in the paraventricular hypothalamus, highlighting its potential impact on neuroinflammatory processes.
Research Applications
HS 014 serves as a valuable tool in neuropharmacological research, particularly in studies investigating the physiological and pathological roles of MC4R. Its high selectivity and potency make it suitable for exploring the receptor's involvement in energy balance, feeding behavior, pain modulation, and neuroinflammation. By employing HS 014, researchers can gain insights into the therapeutic potential of MC4R antagonism in conditions such as obesity, metabolic disorders, and pain syndromes.
Considerations
While HS 014 is a potent MC4R antagonist, its effects on other melanocortin receptor subtypes, though less pronounced, should be considered in experimental designs. Appropriate controls and dosing strategies are essential to delineate the specific contributions of MC4R antagonism in observed outcomes.
In summary, HS 014 is a potent and selective MC4R antagonist that has significantly advanced the understanding of melanocortin receptor physiology and pharmacology. Its application in research continues to provide valuable insights into the complex mechanisms underlying energy homeostasis, feeding behavior, and nociception.
Reference:
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