Product Name:MEN 11270
CAS No:235082-52-7
Purity:95%
Molar Mass:1299.57
Chemical Formula:C60H90N20O11S
Storage:Store at -20 degrees Celsius
Sequence:RRPXGXXXXR
Target:B2 bradykinin receptor
Application:MEN 11270 is a selective antagonist of the B2 bradykinin receptor, which is involved in mediating various physiological responses, such as inflammation, vasodilation, and pain signaling. By blocking the activity of the B2 receptor, MEN 11270 prevents the effects of bradykinin, a peptide that triggers these responses. This antagonist is widely used in research to study the role of bradykinin in conditions like inflammatory diseases, cardiovascular disorders, and pain management. It is a valuable tool for investigating therapeutic strategies aimed at modulating the bradykinin pathway to control inflammation and other related processes.
Current Research:
MEN 11270 is a cyclic decapeptide that functions as a potent and selective antagonist of the human B₂ bradykinin receptor (B₂R). Bradykinin receptors are integral to mediating inflammatory responses, vasodilation, and pain perception. The development of MEN 11270 has provided researchers with a valuable tool to investigate the physiological and pathological roles of B₂R.
Pharmacological Profile
MEN 11270 exhibits high affinity for the B₂R, effectively inhibiting the binding of bradykinin, the receptor's natural ligand. In studies using WI38 human fibroblasts, MEN 11270 demonstrated a pKᵢ value of 10.3, indicating strong binding affinity. Its selectivity is underscored by its minimal interaction with the B₁ bradykinin receptor (B₁R), where it showed a significantly lower affinity (pKᵢ of 6.0). Furthermore, MEN 11270 displayed negligible binding to a range of other receptors and ion channels, highlighting its specificity for B₂R.
Mechanism of Action
As a B₂R antagonist, MEN 11270 competes with bradykinin for receptor binding sites, thereby inhibiting bradykinin-induced physiological effects. This competitive antagonism was evident in human umbilical vein contraction assays, where MEN 11270 caused a concentration-dependent rightward shift in the bradykinin response curve, with a pA₂ value of 8.14.
Applications in Research
The specificity and potency of MEN 11270 make it a valuable tool in exploring the roles of B₂R in various biological processes:
Inflammation and Pain: By blocking B₂R, MEN 11270 helps delineate the receptor's involvement in inflammatory pathways and nociception, aiding in the development of anti-inflammatory and analgesic therapies.
Cardiovascular Studies: Given bradykinin's role in vasodilation and blood pressure regulation, MEN 11270 assists in understanding cardiovascular functions and potential therapeutic targets for hypertension.
Renal Function: Bradykinin influences renal blood flow and sodium excretion; thus, MEN 11270 is utilized to study these processes and their implications in renal pathologies.
Structural Considerations
MEN 11270 is a conformationally constrained derivative of the B₂R antagonist Icatibant. Its cyclic structure is designed to enhance receptor binding affinity and metabolic stability, making it a robust antagonist for in vitro and in vivo studies.
Conclusion
MEN 11270 serves as a potent and selective B₂ bradykinin receptor antagonist, offering significant insights into the receptor's functions across various physiological systems. Its application in research continues to advance our understanding of bradykinin-mediated processes and supports the development of targeted therapeutic interventions.
Reference:
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