MRS2578 is a potent and selective antagonist of the P2Y6 receptor, which is part of the large family of purinergic receptors. It has gained attention for its potential therapeutic use in various inflammatory diseases and cancer. In this article, we will delve into the chemical properties of MRS2578, its health benefits, potential effects, mechanism of action, possible side effects, and dosing information.
Chemical Properties
The chemical name of MRS2578 is 2'-deoxy-N6-methyladenosine-3',5'-bisphosphate butoxymethyl ester. Its molecular formula is C17H22N5O11P2 and formula weight is 567.33 g/mol. The CAS number of MRS2578 is 711019-86-2.
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Health Benefits
MRS2578 has shown potential benefits in treating various inflammatory disorders such as asthma, chronic obstructive pulmonary disease (COPD), colitis, arthritis, and neuroinflammation. Studies have also suggested that it may have anticancer properties by inhibiting tumor growth and inducing cell death in cancer cells.
Potential Effects
MRS2578 primarily acts as an antagonist of the P2Y6 receptor, which is involved in mediating immune responses and inflammation. By blocking this receptor, MRS2578 can reduce inflammation and associated symptoms. Additionally, it has been shown to modulate ATP-induced calcium signaling in cells, indicating its role in extracellular nucleotide signaling pathways.
Product Mechanism
The P2Y6 receptor is activated by extracellular nucleotides such as ATP, leading to downstream signaling pathways that result in inflammation and immune responses. MRS2578 blocks the binding of ATP to the P2Y6 receptor, thereby preventing its activation and downstream signaling. This ultimately reduces the inflammatory response.
Safety
MRS2578 has demonstrated a good safety profile in preclinical studies. However, there is limited information on its safety in humans, and further research is needed to determine its long-term safety and potential toxicities.
Side Effects
There is limited information on the side effects of MRS2578 in humans. However, it is expected to have minimal side effects due to its high selectivity for the P2Y6 receptor.
Dosing Information
MRS2578 has been administered intraperitoneally and intravenously in animal studies at doses ranging from 0.05 to 10 mg/kg. The optimal dose and route of administration for humans are unknown, and further research is needed to establish safe and effective dosing regimens.
Conclusion
MRS2578 is a promising antagonist of the P2Y6 receptor with potential therapeutic applications in various inflammatory diseases and cancer. Its mechanism of action involves blocking extracellular nucleotide signaling pathways, resulting in reduced inflammation. While it has demonstrated a good safety profile in preclinical studies, more research is needed to determine its long-term safety and potential side effects in humans. Nonetheless, MRS2578 has great potential as a novel therapeutic agent in the treatment of inflammatory disorders and cancer.
