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编 号:F143339
分子式:C28H23ClF2N6O3
分子量:564.97
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生物活性:
MRS5698 is a selective Gi protein-coupled A3 adenosine receptor (A3AR) agonist, with Kis of approximately 3 nM for human and mouse A3AR, respectively. MRS5698 can be used for the research of pain and psoriasis.

体内研究:
MRS5698 (3 nmol/day; intrathecal injection for 25 days) prevents Oxaliplatin-induced mechano-allodynia and hyperalgesia, and attenuates Oxaliplatin-induced NLRP3/IL-1β neuroinflammation.MRS5698 (1 mg/kg; i.p. at days 2, 3 ) reduces the IL-23 induced (IL23 injected in day 0, 1, 3) ear thickness of C57BL/6N mouse during the third and fourth experimental days.Animal Model:Oxaliplatin-induced Male Sprague Dawley rats (200–250 g starting weight)
Dosage:3 nmol/day
Administration:Intrathecal injection for 25 days
Result:Increased the value of mechanical paw withdrawal threshold in grams (PWT) in rat.Attenuated oxaliplatin-induced expression of NLRP3 and maturation of caspase 1 in the DH-SC.Reduced IL-1β levels in the spinal cord.

体外研究:
MRS5698 displays higher affinity and selectivity (>3000-fold) agonist A3R vs. other adenosine receptor (ARs) in both human and mouse.MRS5698 (0.1-10 μM; 1 hours) induces a concentration-dependently robust A3R-mediated cAMP reduction in HEK-293T cells permanently expressing the A3R, regardless the illumination condition.
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