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  3. PTUPB

PTUPB 

Cat. No.: HY-122591
Handling Instructions

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

For research use only. We do not sell to patients.

PTUPB Chemical Structure

PTUPB Chemical Structure

CAS No. : 1287761-01-6

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Description

PTUPB is a potent and dual sEH and COX-2 enzymes inhibitor with IC50 of 0.9 nM and 1.26 μM, respectively[1].

IC50 & Target[3]

COX-1

1.26 μM (IC50)

COX-1

100 μM (IC50)

sEH

0.9 nM (IC50)

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[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].

Cell Viability Assay[1]

Cell Line: Multiple cancer cell lines: PC-3 cells, Met-1, H-1, A375, and transformed endothelial cell line (bEnd.3)
Concentration: 10 μM, 15 μM, and 20 μM
Incubation Time: 72 hours
Result: Inhibited HUVEC proliferation after 3 days.

Cell Cycle Analysis[1]

Cell Line: HUVECs
Concentration: 10 μM, 15 μM, and 20 μM
Incubation Time: 72 hours
Result: Induced cell cycle arrest at the G0/1 phase.
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[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].

Animal Model: C57BL/6 mice with LLC cells[1]
Dosage: 30 mg/kg; 4 weeks
Administration: Subcutaneous injection via Alzet osmotic minipumps; once daily; 4 weeks
Result: Inhibited LLC tumor growth and metastasis.
Animal Model: High-fat diet (HFD)-induced obeseadult male C57BL/6 mice[2]
Dosage: 5 mg/kg; 12 weeks
Administration: Subcutaneous injection; once daily; 12 weeks
Result: Arrested fibrotic progression and ameliorated high-fat diet-induced non-alcoholic fatty liver disease.
Molecular Weight

543.56

Formula

C₂₆H₂₄F₃N₅O₃S

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

PTUPBCOXCyclooxygenaseNon-alcoholicfattyliverdiseaseobesityHFDMetastasisHUVECshepaticsteatosisLLCInhibitorinhibitorinhibit

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