PTUPB

PTUPB is a potent and dual sEH and COX-2 enzymes inhibitor with IC50 of 0.9 nM and 1.26 μM, respectively.

Product information

CAS Number: 1287761-01-6

Molecular Weight: 543.56

Formula: C26H24F3N5O3S

Chemical Name: 3-{3-[5-phenyl-1-(4-sulfamoylphenyl)-1H-pyrazol-3-yl]propyl}-1-[4-(trifluoromethyl)phenyl]urea

Smiles: NS(=O)(=O)C1C=CC(=CC=1)N1N=C(CCCNC(=O)NC2C=CC(=CC=2)C(F)(F)F)C=C1C1C=CC=CC=1

InChiKey: CSEPEVFNTFMBAE-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (183.97 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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. 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. 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.

In Vivo:

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. 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.

Products are for research use only. Not for human use.