GLPBio

PTUPB

Catalog No.: GC60311Purity:>98.00%
COASDSData Sheet
PTUPB is a novel dual COX-2 and sEH inhibitor with IC50 values of 1.26 nM and 0.9 μM, respectively.

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PTUPB
Cas No.: 1287761-01-6
10mM (in 1mL DMSO)In Stock
$84.00
1
1mgIn Stock
$27.00
1
5mgIn Stock
$70.00
1
10mgIn Stock
$118.00
1
25mgIn Stock
$220.00
1
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Description

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.

Protocol

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.
Enzymes (∼1 nM human sEH) were incubated with PTUPB for 5 min in 25 mM Bis-Tris/HCl buffer (200 μL; pH 7.0) at 30 °C before substrate (cyano(2-methoxynaphthalen-6-yl)methyl trans-(3-phenyl-oxyran-2-yl)methyl carbonate (CMNPC) was added.
Activity was assessed by measuring the appearance of the fluorescent 6-methoxynaphthaldehyde product (λem= 330 nm, λex = 465 nm) at 30 ℃ during a 10 min incubation.

Applications

 PTUPB is sEH inhibitor with IC50 values of 0.9 μM.

References:
[1]. 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.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
1287761-01-6
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
Molecular Formula
C26H24F3N5O3S
Molecular Weight
543.56
Solubility
DMSO: 100 mg/mL (183.97 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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