PTUPB |
| Catalog No.GC60311 |
PTUPB is a novel dual COX-2 and sEH inhibitor with IC50 values of 1.26 nM and 0.9 μM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1287761-01-6
Sample solution is provided at 25 µL, 10mM.
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PTUPB is a novel dual COX-2 and sEH inhibitor with IC50 values of 1.26 nM and 0.9 μM, respectively[1]. It has certain anti-tumor and anti-inflammatory effects[2].
PTUPB(10, 100, 1000, and 10000 nM;1h) inhibits the activation of NLRP3 inflammasome in primary murine macrophages by reduced the protein expression of caspase-1 p10 and IL-1β p17 in macrophages [3]. PTUPB (10, 20, 25 or 30 μM; 72 h) inhibits glioblastoma cell proliferation and G1 phase cell cycle arrest in vitro, and suppresses the tumor growth and angiogenesis in vivo[4].
PTUPB(5 mg/kg; 1 h before the LPS administration; s.c) decreased the pro-inflammatory factors, oxidative stress, and activation of NACHT, LRR, and PYD domains-containing protein 3 (NLRP3) inflammasome in LPS-induced ALI mice [3]. PTUPB(10 mg/kg/d; 8 weeks) attenuates renal inflammation and oxidative stress in Zucker diabetic fatty(ZDF) rats[5]. PTUPB(5 mg/kg; s.c) treatment suppressed the activation of NLRP3 inflammasome in the liver and lung of septic mice[6]. PTUPB (5 mg/kg; s.c; once a day for 14days) alleviated the pathological changes in lung tissue and collagen deposition, as well as reduced senescence marker molecules (p16Ink4a and p53-p21Waf1/Cip1) in the lungs of mice treated by bleomycin (BLM) [7].
References:
[1]. Hwang SH, Wagner KM, et,al. Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase. J Med Chem. 2011 Apr 28;54(8):3037-50. doi: 10.1021/jm2001376. Epub 2011 Apr 5. PMID: 21434686; PMCID: PMC3281519.
[2]. Wang F, Zhang H, et,al. COX-2/sEH Dual Inhibitor PTUPB Potentiates the Antitumor Efficacy of Cisplatin. Mol Cancer Ther. 2018 Feb;17(2):474-483. doi: 10.1158/1535-7163.MCT-16-0818. Epub 2017 Dec 28. PMID: 29284644; PMCID: PMC5824635.
[3]. Yang HH, Duan JX, et,al. A COX-2/sEH dual inhibitor PTUPB alleviates lipopolysaccharide-induced acute lung injury in mice by inhibiting NLRP3 inflammasome activation. Theranostics. 2020 Mar 26;10(11):4749-4761. doi: 10.7150/thno.43108. PMID: 32308747; PMCID: PMC7163435.
[4]. Li J, Zhou Y, et,al. COX-2/sEH dual inhibitor PTUPB suppresses glioblastoma growth by targeting epidermal growth factor receptor and hyaluronan mediated motility receptor. Oncotarget. 2017 Sep 15;8(50):87353-87363. doi: 10.18632/oncotarget.20928. PMID: 29152086; PMCID: PMC5675638.
[5]. Hye Khan MA, Hwang SH, et,al. A dual COX-2/sEH inhibitor improves the metabolic profile and reduces kidney injury in Zucker diabetic fatty rat. Prostaglandins Other Lipid Mediat. 2016 Sep;125:40-7. doi: 10.1016/j.prostaglandins.2016.07.003. Epub 2016 Jul 16. PMID: 27432695; PMCID: PMC5035206.
[6]. Zhang YF, Sun CC, et,al. A COX-2/sEH dual inhibitor PTUPB ameliorates cecal ligation and puncture-induced sepsis in mice via anti-inflammation and anti-oxidative stress. Biomed Pharmacother. 2020 Jun;126:109907. doi: 10.1016/j.biopha.2020.109907. Epub 2020 Feb 27. PMID: 32114358; PMCID: PMC8868492.
[7]. Zhang CY, Duan JX, et,al. COX-2/sEH dual inhibitor PTUPB alleviates bleomycin-induced pulmonary fibrosis in mice via inhibiting senescence. FEBS J. 2020 Apr;287(8):1666-1680. doi: 10.1111/febs.15105. Epub 2019 Nov 8. PMID: 31646730; PMCID: PMC7174142.
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