HS 024

Product Name:HS 024

CAS No:212370-59-7

Purity:95%

Molar Mass:1266.5

Chemical Formula:C58H79N19O10S2

Storage:Store at -20 degrees Celsius

Sequence:CXRHXRWGC

Target:melanocortin-4 receptor (MC4R)

Application:

HS 024 is a selective melanocortin-4 receptor (MC4R) antagonist, commonly utilized in research to explore the physiological and pathological roles of MC4R in energy balance, appetite control, and metabolic regulation. By blocking MC4R activity, HS 024 is instrumental in studies investigating the mechanisms underlying obesity, metabolic syndrome, and other related disorders. This peptide's high specificity for MC4R ensures targeted inhibition, providing researchers with precise control in experimental setups. With its high purity and consistent performance, HS 024 is an essential tool for neuroendocrinology and metabolic research, offering insights into the modulation of energy homeostasis.

Current Research:

HS 024 (CAS: 212370-59-7) is a synthetic peptide that functions as a highly potent and selective antagonist of the melanocortin-4 receptor (MC4R), a G protein-coupled receptor involved in regulating energy homeostasis, feeding behavior, and cardiovascular functions. The peptide exhibits high affinity for MC4R, with a Ki value of 0.29 nM, and demonstrates significantly lower affinities for other melanocortin receptor subtypes, including MC1R (Ki = 18.6 nM), MC3R (Ki = 5.45 nM), and MC5R (Ki = 3.29 nM), underscoring its selectivity.
Chemical Structure and Properties
HS 024 has the sequence Ac-Cys-Nle-Arg-His-D-2-Nal-Arg-Trp-Gly-Cys-NH?, where Nle represents norleucine and D-2-Nal denotes 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 9, contributing to its conformational stability. It has a molecular weight of 1266.5 g/mol and is soluble in water up to 0.5 mg/mL.
Pharmacological Effects
In vivo studies have demonstrated that central administration of HS 024 increases food intake in rats, indicating its role in modulating appetite through MC4R antagonism. Additionally, HS 024 has been shown to block ??-MSH- and MTII-induced hypotension and bradycardia in rats, suggesting its involvement in cardiovascular regulation.
Research Applications
HS 024 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, and cardiovascular functions. By employing HS 024, researchers can gain insights into the therapeutic potential of MC4R antagonism in conditions such as obesity, metabolic disorders, and cardiovascular diseases.
Considerations
While HS 024 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 024 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 cardiovascular regulation.

Reference:

Turcic, P., Stambuk, N., Konjevoda, P., Kelava, T., Gabricevic, M., Stojkovic, R., & Aralica, G. (2015). Modulation of ??2-MSH hepatoprotection by antisense peptides and melanocortin subtype 3 and 4 receptor antagonists. Medicinal chemistry, 11(3), 286-295