NF340 is a P2Y11 receptor inhibitor with a pIC50 of 7.3-7.7 against human P2Y11 receptor, and it exhibits high selectivity over other P2Y family receptors. NF340 binds to the ATP-binding amino acid residues of the P2Y11 receptor to inhibit its activity, block nociceptive activity, and reduce spinal dorsal horn P2Y11 receptor upregulation induced by spinal cord injury. NF340 attenuates the NFkappaB signaling pathway activated by IL-1beta by decreasing IkappaBalpha phosphorylation, nuclear p65 accumulation and NFkappaB promoter activity. NF340 inhibits IL-1beta-induced pro-inflammatory cytokine expression, reduces intracellular ROS and 4-HNE levels, and suppresses IL-1beta-induced matrix metalloproteinase expression in primary fibroblast-like synoviocytes. NF340 inhibits ATP-induced elevation of intracellular calcium 2+ concentration and cell migration in human hepatocellular carcinoma cells. NF340 is applicable to the research of neuropathic pain, myocardial ischemia/reperfusion injury, inflammatory pain, rheumatoid arthritis and hepatocellular carcinoma[1][2][3][4][5].
Molecular Weight:
986.84
CAS Number:
[202982-98-7]
Formula:
C37H26N4Na4O15S4
Target:
P2Y Receptor
Application Notes:
MCE Product type: Reference compound
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