PTUPB

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PTUPB 是一种新型双重作用 COX-2/sEH 抑制剂，IC50 为 1.26 uM/0.9 nM。

PTUPB is a novel dual acting COX-2/sEH inhibitor with IC50 of 1.26 uM/0.9 nM,does not inhibits COX-1 (IC50>100 uM); reduces kidney injury parameters, decreases inflammatory and oxidative stress markers in ZDF rats; exhibits more effective than the same dose of either COX-2 inhibitor (celecoxib) or sEH inhibitor (t-AUCB) alone, shows in vivo antiallodynic activity in vivo; also suppresses glioblastoma growth by targeting EGFR and hyaluronan mediated motility receptor, potentiates the antitumor efficacy of cisplatin.

Cell Viability Assay 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 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.

Animal Model:C57BL/6 mice with?LLC cells 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 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.

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Chromatin/Epigenetic

COX

COX

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1287761-01-6

543.565

C26H24F3N5O3S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (183.97 mM)

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4-(5-phenyl-3-{3-[3-(4-trifluoromethylphenyl)-ureido]-propyl}-pyrazol-1-yl)-benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years