Product Name:MM 54
CAS No:1313027-43-8
Purity:95%
Molar Mass:1737.16
Chemical Formula:C70H121N29O15S4
Storage:Store at -20 degrees Celsius
Sequence:CRPRLCKHCRPRLC
Target:APJ receptor agonist
Application:
MM 54 is related to the APJ receptor (also known as the apelin receptor) and acts as an agonist for this receptor. The APJ receptor is a G protein-coupled receptor involved in various physiological processes, including cardiovascular regulation, fluid homeostasis, and energy metabolism. Activation of the APJ receptor by agonists like MM 54 influences blood pressure, heart contractility, and vascular tone. This makes MM 54 useful in research focused on cardiovascular health, heart failure, and metabolic conditions. It also provides insights into the role of the apelin/APJ signaling pathway in potential therapeutic interventions for cardiovascular diseases and metabolic disorders.
Current Research:
MM 54 (CAS: 1313027-43-8) is a synthetic cyclic peptide that functions as a potent and selective antagonist of the apelin receptor (APJ), a G protein-coupled receptor involved in various physiological processes, including cardiovascular regulation, fluid homeostasis, and energy metabolism. By inhibiting APJ, MM 54 modulates the apelinergic system, offering potential therapeutic applications in conditions such as heart failure, hypertension, and cancer.
Chemical Structure and Properties
MM 54 is composed of 14 amino acids with the sequence Cys-Arg-Pro-Arg-Leu-Cys-Lys-His-Cys-Arg-Pro-Arg-Leu-Cys. It features two disulfide bridges between Cys¹-Cys⁶ and Cys⁹-Cys¹⁴, forming a cyclic structure that enhances its stability and receptor affinity. The molecular formula is C₇₀H₁₂₁N₂₉O₁₅S₄, and it has a molecular weight of approximately 1737.15 Da.
Mechanism of Action
MM 54 acts as a competitive antagonist at the apelin receptor, with a dissociation constant (Kᵢ) of 82 nM and an inhibitory concentration (IC₅₀) of 93 nM. It effectively blocks the binding of endogenous apelin peptides, such as [Pyr¹]-Apelin-13, thereby inhibiting downstream signaling pathways. In cellular assays, MM 54 antagonizes the inhibitory effect of [Pyr¹]-Apelin-13 on forskolin-induced cAMP accumulation in CHO-K1 cells expressing APJ.
Pharmacological Effects
In preclinical studies, MM 54 has demonstrated significant biological activity:
Antitumor Activity: In a mouse xenograft model of glioblastoma, MM 54 reduced tumor expansion and prolonged survival time, indicating its potential as an anticancer agent.
Research Applications
MM 54 serves as a valuable tool in biomedical research for:
Investigating Apelinergic Signaling: By selectively inhibiting APJ, researchers can study the physiological and pathological roles of apelin and its receptor in various systems.
Developing Therapeutic Agents: MM 54 provides a structural framework for designing new drugs targeting the apelin receptor, with potential applications in treating cardiovascular diseases, metabolic disorders, and cancers.
Handling and Storage
MM 54 is typically supplied as a lyophilized powder. For optimal stability, it should be stored at -20°C, protected from light and moisture. Upon reconstitution, solutions can be prepared in water or dimethyl sulfoxide (DMSO), with solubility up to 2 mg/mL in water.
Conclusion
As a potent and selective apelin receptor antagonist, MM 54 offers significant potential in both research and therapeutic contexts. Its ability to modulate APJ activity makes it a promising candidate for developing treatments targeting the apelinergic system in various diseases.
Reference:
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