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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- CAS 番号: 202982-98-7
- 分子式: C37H26N4Na4O15S4
- 分子量:986.84
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
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生物活性
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P2Y11 Receptor |
NF340 inhibits the P2Y11R-mediated modulation of adult ventricular human CF secretome, abolishing the NF546-induced reduction in human DC maturation marker expression and reducing the NF546-induced protective effect on human cardiomyocyte viability after simulated I/R injury[2].
NF340 is a selective antagonist of human P2Y11 receptors, with a pEC50 of 7.3-7.7, showing 1000-fold lower potency at other human P2Y receptor subtypes[3].
NF340 (10-20 μM; 24 h) dose-dependently inhibits IL-1β-induced TNF-α and IL-6 expression at both mRNA and protein levels in human fibroblast-like synoviocytes, with 20 μM NF340 exerting a stronger inhibitory effect than 10 μM NF340[4].
NF340 (10-20 μM; 24 h) dose-dependently inhibits IL-1β-induced MMP-1, MMP-3, and MMP-13 expression at both mRNA and protein levels in human fibroblast-like synoviocytes, with 20 μM NF340 exerting a stronger inhibitory effect than 10 μM NF340[4].
NF340 (10-20 μM; 24 h) dose-dependently ameliorates IL-1β-induced oxidative stress in human fibroblast-like synoviocytes, as measured by reduced cellular ROS and 4-HNE levels, with 20 μM NF340 exerting a stronger inhibitory effect than 10 μM NF340[4].
NF340 (10-20 μM; 6 h (p-IκBα assay); 24 h (nuclear p65 and luciferase assays)) dose-dependently inhibits IL-1β-induced NF-κB activation in human fibroblast-like synoviocytes, as measured by reduced IκBα phosphorylation, nuclear p65 accumulation, and NF-κB promoter activity, with 20 μM NF340 exerting a stronger inhibitory effect than 10 μM NF340[4].
NF340 (10 μM; 5 min) potently inhibits ATP-induced intracellular calcium elevation in Huh-7 human hepatocellular carcinoma cells[5].
NF340 (10 μM; 5 min) significantly reduces NF546-induced intracellular calcium elevation in HepG2 human hepatocellular carcinoma cells[5].
NF340 (10 μM; 24 h) completely blocks ATP-induced migration of Huh-7 human hepatocellular carcinoma cells without affecting basal migration[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human fibroblast-like synoviocytes (FLS)
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Concentration:10 μM, 20 μM
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Incubation Time:24 h
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Result:Reduced IL-1β-induced TNF-α mRNA expression from 5.8-fold to 3.5-fold at 10 μM, and to 2.2-fold at 20 μM.
Reduced IL-1β-induced IL-6 mRNA expression from 4.5-fold to 3-fold at 10 μM, and to 1.5-fold at 20 μM.
Reduced IL-1β-induced TNF-α protein induction from 5-fold to 3-fold at 10 μM, and to 1.7-fold at 20 μM.
Reduced IL-1β-induced IL-6 protein induction from 4.2-fold to 2.8-fold at 10 μM, and to 1.5-fold at 20 μM.\nReduced IL-1β-induced MMP-1, MMP-3, and MMP-13 mRNA expression from 5-6-fold to 3-fold at 10 μM, and to 2-fold at 20 μM.
Reduced IL-1β-induced MMP-1, MMP-3, and MMP-13 protein expression from 4-5-fold to 3-fold at 10 μM, and to 2-fold at 20 μM.
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Cell Line:human fibroblast-like synoviocytes (FLS)
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Concentration:10 μM (p-IκBα assay); 20 μM (p-IκBα assay); 10 μM (nuclear p65 and luciferase assays); 20 μM (nuclear p65 and luciferase assays)
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Incubation Time:6 h (p-IκBα assay); 24 h (nuclear p65 and luciferase assays)
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Result:Reduced IL-1β-induced p-IκBα phosphorylation from 5-fold to 3.5-fold at 10 μM (6 h), and to 2-fold at 20 μM (6 h).
Reduced IL-1β-induced nuclear p65 accumulation from 3.2-fold to 2-fold at 10 μM (24 h), and to 1.5-fold at 20 μM (24 h).
Reduced IL-1β-induced NF-κB luciferase promoter activity from 80-fold to 50-fold at 10 μM (24 h), and to 25-fold at 20 μM (24 h).
NF340 (1-10 nmol/paw; s.c.; 10 minutes before formalin injection) produces peripherally localized antinociception in the second phase of formalin-induced inflammatory pain in female Wistar rats[3].
NF340 (1 nmol/paw; s.c.; co-administered with P2Y11 receptor agonists; 10 minutes before formalin injection) blocks P2Y11 agonist-induced pronociception in formalin-induced inflammatory pain in female Wistar rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (female, 140-180 g, left L5 and L6 spinal nerve ligation)[1]
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Dosage:0.3 μM (single injection antiallodynia); 10 μM (single injection antiallodynia); 30 μM (single injection antiallodynia; repeated injection P2Y11 regulation)
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Administration:i.t.; single bolus injection; 6-hour assessment period; i.t.; every 12 hours; 3 days
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Result:Produced significant, dose-dependent antiallodynic effects, increasing 50% paw withdrawal thresholds in spinal nerve ligated rats, with maximal effect reached at ~1 hour and decaying gradually over 6 hours.
Reversed spinal nerve injury-induced up-regulation of P2Y11 receptor expression in the ipsilateral dorsal spinal cord, reducing relative P2Y11/β-actin intensity from ~1.4 to ~0.4.
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Animal Model:Wistar rats (female, 8-10 weeks old, 180-200 g, inflammatory pain model via 1% formalin injection)[3]
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Dosage:1 nmol/paw; 10 nmol/paw
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Administration:s.c.; 10 minutes before formalin injection
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Result:Significantly reduced 1% formalin-induced flinching behavior during the second phase (15-60 minutes) of the test.
Did not affect formalin-induced nociception in any phase when administered contralaterally.
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Animal Model:Wistar rats (female, 8-10 weeks old, 180-200 g, inflammatory pain model via 0.5% formalin injection)[3]
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Dosage:1 nmol/paw
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Administration:s.c.; co-administered with P2Y11 receptor agonists, 10 minutes before formalin injection
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Result:Prevented the pronociceptive effect induced by ATP (1000 nmol/paw) in both phases of the formalin test.
Prevented the pronociceptive effect induced by NF546 (3 nmol/paw) during the second phase of the test.
Did not modify 0.5% formalin-induced nociceptive behavior when administered alone at this dose.
化学情報
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CAS 番号 202982-98-7
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分子量 986.84
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分子式 C37H26N4Na4O15S4
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
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データシート (284 KB)
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- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
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- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[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]
Calculators
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NF340 関連分類
HY-108659 関連分類
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- NF340
- 202982-98-7
- NF 340
- NF-340
- P2Y Receptor
- Interleukin Related
- NF-κB
- Reactive Oxygen Species (ROS)
- fibroblast-like synoviocytes
- NFκB signaling
- dendritic cell
- IκBα phosphorylation
- dorsal spinal cord
- P2Y11 receptor
- cardiomyocytes
- spinal nerve ligated rats
- human hepatocellular carcinoma cells
- cardiac fibroblast
- Inhibitor
- inhibitor
- inhibit