202982-98-7
Chemical Structure
NF340
- CAS No.: 202982-98-7
- Formula:C37H26N4Na4O15S4
- Molecular Weight:986.84
IUPAC Name: sodium 4,4'-((3,3'-(carbonylbis(azanediyl))bis(4-methylbenzoyl))bis(azanediyl))bis(naphthalene-2,6-disulfonate)
InChIKey: SJMHXBFWMZYDBY-UHFFFAOYSA-J
SMILES: O=C(NC1=CC(C(NC2=C3C=C(S(=O)(O[Na])=O)C=CC3=CC(S(=O)(O[Na])=O)=C2)=O)=CC=C1C)NC4=CC(C(NC5=C6C=C(S(=O)(O[Na])=O)C=CC6=CC(S(=O)(O[Na])=O)=C5)=O)=CC=C4C
Biological Activity: 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 nerve injury. NF340 attenuates the NFκB signaling pathway activated by IL-1β by decreasing IκBα phosphorylation, nuclear p65 accumulation, and NFκB promoter activity. NF340 inhibits IL-1β-induced pro-inflammatory cytokine expression, reduces intracellular ROS and 4-HNE levels, and suppresses IL-1β-induced matrix metalloproteinase expression in primary fibroblast-like synoviocytes. NF340 inhibits ATP-induced elevation of intracellular Ca2+ concentration and cell migration in human hepatocellular carcinoma cells. NF340 can be used in the research of neuropathic pain, myocardial ischemia/reperfusion injury, inflammatory pain, rheumatoid arthritis, and hepatocellular carcinoma[1][2][3][4][5].
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NF340 | 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 nerve injury. NF340 attenuates the NFκB signaling pathway activated by IL-1β by decreasing IκBα phosphorylation, nuclear p65 accumulation, and NFκB promoter activity. NF340 inhibits IL-1β-induced pro-inflammatory cytokine expression, reduces intracellular ROS and 4-HNE levels, and suppresses IL-1β-induced matrix metalloproteinase expression in primary fibroblast-like synoviocytes. NF340 inhibits ATP-induced elevation of intracellular Ca2+ concentration and cell migration in human hepatocellular carcinoma cells. NF340 can be used in the research of neuropathic pain, myocardial ischemia/reperfusion injury, inflammatory pain, rheumatoid arthritis, and hepatocellular carcinoma. | |||||||||||||||||||||
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- [1]. Barragán-Iglesias P, et al. Role of spinal P2Y6 and P2Y11 receptors in neuropathic pain in rats: possible involvement of glial cells. Mol Pain. 2014;10:29. Published 2014 May 20. [Content Brief]
- [2]. Lefort C, et al. Stimulation of P2Y11 receptor modulates cardiac fibroblasts secretome toward immunomodulatory and protective roles after Hypoxia/Reoxygenation injury. J Mol Cell Cardiol. 2018 Aug;121:212-222. [Content Brief]
- [3]. Barragán-Iglesias P, et al. Participation of peripheral P2Y1, P2Y6 and P2Y11 receptors in formalin-induced inflammatory pain in rats. Pharmacol Biochem Behav. 2015;128:23-32. [Content Brief]
- [4]. Gao F, et al. P2Y11 receptor antagonist NF340 ameliorates inflammation in human fibroblast-like synoviocytes: An implication in rheumatoid arthritis. IUBMB Life. 2019;71(10):1552-1560. [Content Brief]
- [5]. Khalid M, et al. Carcinoma-specific expression of P2Y11 receptor and its contribution in ATP-induced purinergic signalling and cell migration in human hepatocellular carcinoma cells. Oncotarget. 2017;8(23):37278-37290. [Content Brief]
Keywords
