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编 号:F326942
分子式:C12H18N2O
分子量:206.28
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
HET0016 is a potent and selective 20-hydroxyeicosatetraenoic acid (20-HETE) synthase inhibitor, with IC50 values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis, respectively. HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth.

体内研究:
HET0016 (10 mg/kg/day; i.v.; for 3 weeks) reduces tumor volume and lung metastasis in an immunocompetent breast cancer mouse model.HET0016 reduces the metalloproteinases’ levels in the lungs via PI3K/AKT pathway in mice.HET0016 decreases expression of pro-inflammatory and growth factors and granulocytic MDSCs population in lung microenvironment.HET0016 protects BBB dysfunction after I/R by regulating the expression of MMP-9 and tight junction proteins.Animal Model:4–5 weeks female Balb/c mice (16-18 g)
Dosage:10 mg/kg/day
Administration:Intravenously; 5 days a week; for 3 weeks; starting from day 15 of tumor implantation
Result:Reduced tumor volume and lung metastasis.

体外研究:
HET0016 is a selective, non-competitive and irreversible inhibitor of CYP4A .HET0016 (100 μM; 24 hours, 48 hours) decreases migration and invasion of breast cancer metastatic cells .
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