PG 931

Product Name:PG 931

CAS No:667430-81-1

Purity:95%

Molar Mass:1180.4

Chemical Formula:C59H85N15O11

Storage:Store at -20 degrees Celsius

Sequence:Ac-{Nle}-DP-{D-Phe}-RWKPV-NH2

Target:melanocortin 4 (MC4) receptor

Application:PG 931 is a selective antagonist of the melanocortin 4 (MC4) receptor, which plays a critical role in regulating energy homeostasis, appetite, and body weight. The MC4 receptor is part of the melanocortin system, which influences a range of physiological processes, including feeding behavior, metabolism, and sexual function. By blocking the MC4 receptor, PG 931 is valuable in research focused on obesity, metabolic disorders, and conditions related to energy balance and appetite control. Its ability to inhibit MC4 receptor activity makes it a useful tool in studying the therapeutic potential for managing obesity and related metabolic diseases.

Current Research:

PG 931 (CAS: 667430-81-1) is a synthetic peptide that functions as a potent and selective agonist of the melanocortin 4 receptor (MC4R), a G protein-coupled receptor involved in regulating energy homeostasis, feeding behavior, and cardiovascular functions. Its high affinity and specificity make it a valuable tool for research into MC4R-related physiological and pathological processes.
Structural Characteristics
PG 931 is an analog of the peptide SHU 9119, with the sequence Ac-Nle-cyclo[Asp-Pro-D-Phe-Arg-Trp-Lys]-Pro-Val-NH?. This structure includes a lactam bridge between Asp2 and Lys?, contributing to its conformational stability and receptor selectivity.
Pharmacological Profile
PG 931 exhibits high potency and selectivity for MC4R, with an IC?? of 0.58 nM. It shows significantly lower affinity for the melanocortin 3 receptor (MC3R) and melanocortin 5 receptor (MC5R), with IC?? values of 55 nM and 2.4 nM, respectively.
Mechanism of Action
As an MC4R agonist, PG 931 binds to the receptor, activating downstream signaling pathways that influence various physiological functions, including energy balance, appetite regulation, and cardiovascular responses.
Research Applications
PG 931 is utilized in preclinical studies to investigate the role of MC4R in:
Energy Homeostasis and Obesity: Understanding how MC4R activation affects feeding behavior and energy expenditure, which is crucial for developing obesity treatments.
Cardiovascular Function: Exploring the receptor's involvement in blood pressure regulation and heart rate control.
Hemorrhagic Shock: Evaluating its potential therapeutic effects in restoring cardiovascular and respiratory functions following severe blood loss. In animal models, PG 931 has demonstrated rapid, dose-dependent restoration of these functions in hemorrhage-shocked rats.
Conclusion
PG 931 serves as a potent and selective MC4R agonist, offering significant utility in research focused on metabolic disorders, cardiovascular diseases, and potential therapeutic interventions targeting the melanocortin system.

Reference:

Giuliani, D., Mioni, C., Bazzani, C., Zaffe, D., Botticelli, A. R., Capolongo, S., ... & Guarini, S. (2007). Selective melanocortin MC4 receptor agonists reverse haemorrhagic shock and prevent multiple organ damage. British Journal of Pharmacology, 150(5), 595-603.