For research use only. Not for therapeutic Use.
PTUPB is a potent and dual sEH and COX-2 enzymes inhibitor with IC50 of 0.9 nM and 1.26 μM, respectively[1].
PTUPB (1-10 μM; 24 hours) shows an inhibitory activity against human 5-LOX, exhibits a 83% and 44% inhibition at 10 μM and 1 μM, respectively[1].PTUPB (10-20 μM; 72 hours) has minimal inhibitory effects on cell proliferation in multiple cancer cell lines, including human melanoma cell and a transformed endothelial cell, whereas it potently inhibits HUVEC proliferation after 3 days of application[1].PTUPB (10-20 μM; 72 hours) induces cell cycle arrest at the G0/1 phase at different various. The percentage of cell number of PTUPB are 65.15%, 66.87%,and 65.91% at 10 μM, 15 μM, and 20 μM, respectively[1].
PTUPB (subcutaneous injection; 30 mg/kg; 4 weeks) inhibits LLC tumor growth by 70-83% and exhibits with no overt toxicity, such as any weight loss when it is compared with the control group. After a period of treatment, the peak plasma concentration of PTUPB is high[1].PTUPB (subcutaneous injection; 5 mg/kg; once daily; 12 weeks) ameliorates high-fat diet-induced non-alcoholic fatty liver disease via inhibiting NLRP3 inflammasome activation. It reduces body weight, liver weight, liver triglyceride and cholesterol content. It also decreases the expression of lipolytic/lipogenic and lipid uptake related genes[2].
| Catalog Number | I015546 |
| CAS Number | 1287761-01-6 |
| Synonyms | 1-[3-[5-phenyl-1-(4-sulfamoylphenyl)pyrazol-3-yl]propyl]-3-[4-(trifluoromethyl)phenyl]urea |
| Molecular Formula | C26H24F3N5O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C26H24F3N5O3S/c27-26(28,29)19-8-10-20(11-9-19)32-25(35)31-16-4-7-21-17-24(18-5-2-1-3-6-18)34(33-21)22-12-14-23(15-13-22)38(30,36)37/h1-3,5-6,8-15,17H,4,7,16H2,(H2,30,36,37)(H2,31,32,35) |
| InChIKey | CSEPEVFNTFMBAE-UHFFFAOYSA-N |
| SMILES | C1=CC=C(C=C1)C2=CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)CCCNC(=O)NC4=CC=C(C=C4)C(F)(F)F |
| Reference | [1]. Sun CC, et al. PTUPB ameliorates high-fat diet-induced non-alcoholic fatty liver disease via inhibiting NLRP3 inflammasome activation in mice. Biochem Biophys Res Commun. 2020 Mar 19;523(4):1020-1026. [2]. Zhang G, et al. Dual inhibition of cyclooxygenase-2 and soluble epoxide hydrolase synergistically suppresses primary tumor growth and metastasis. Proc Natl Acad Sci U S A. 2014 Jul 29;111(30):11127-32. [3]. Hwang SH, 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. |
