PTUPB |
| رقم الكتالوجGC60311 |
PTUPB هو مثبط قوي وثنائي لإنزيمات sEH و COX-2 مع IC50 0.9 نانومتر و 1.26 ميكرومتر على التوالي
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.
| Cell experiment [1]: | |
|
Cell lines |
Primary murine peritoneal macrophages |
|
Preparation Method |
Macrophages were treated with LPS (100 ng/mL) for 6 h with or without PTUPB pre-treatment (10, 100, and 1000 nM) for 1 h and activity of LDH in the supernatant was detected. |
|
Reaction Conditions |
10, 100, 1000, and 10000 nM;1h |
|
Applications |
PTUPB pretreatment at concentrations of 10, 100, and 1000 nM significantly decreased the LDH activity triggered by LPS. |
| Animal experiment [1]: | |
|
Animal models |
Acute lung injury (ALI) C57BL/6 mice |
|
Preparation Method |
Mice were subcutaneously injected with PTUPB (5 mg/kg) dissolved in PEG400 1 h prior to ALI. Specifically, The mice were randomly assigned to four groups: control, PTUPB, ALI, and ALI + PTUPB. ALI was induced by administering an intratracheal injection of LPS (5 mg/kg) dissolved in 50 μL of sterile saline. Mice in the PTUPB and PTUPB + ALI groups received a subcutaneous injection of PTUPB (5 mg/kg) dissolved in PEG400, one hour before the intratracheal injection. For the control and ALI groups, PEG400 was administered subcutaneously. |
|
Dosage form |
5 mg/kg; 1 h before the LPS administration (ALI); s.c |
|
Applications |
PTUPB mitigates the pathological lung damage and restores the respiratory function in mice exposed to LPS. |
| Kinase experiment [1]: | |
|
Preparation Method |
For the recombinant affinity purified sEHs (human, mouse, and rat), we used a fluorescent-based assay to determine IC50s. |
|
Applications |
PTUPB is sEH inhibitor with IC50 values of 0.9 μM. |
|
References: |
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| Cas No. | 1287761-01-6 | SDF | |
| Canonical SMILES | O=S(C1=CC=C(N2N=C(CCCNC(NC3=CC=C(C(F)(F)F)C=C3)=O)C=C2C4=CC=CC=C4)C=C1)(N)=O | ||
| Formula | C26H24F3N5O3S | M.Wt | 543.56 |
| الذوبان | DMSO: 100 mg/mL (183.97 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8397 mL | 9.1986 mL | 18.3972 mL |
| 5 mM | 0.3679 mL | 1.8397 mL | 3.6794 mL |
| 10 mM | 0.184 mL | 0.9199 mL | 1.8397 mL |
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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