1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHET0016Cat. No.: HY-124527CAS No.: 339068-25-6分式: CHNO分量: 206.28作靶點: Cytochrome P450作通路: Metabolic Enzyme/Protease儲存式: Please store the product under the recommended conditions inthe COA.溶解性數(shù)據(jù)體外實驗 DMSO : 5 mg/mL (24.24 mM; Need

2、ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 4.8478 mL 24.2389 mL 48.4778 mL5 mM 0.9696 mL 4.8478 mL 9.6956 mL10 mM 0.4848 mL 2.4239 mL 4.8478 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 HET0016種效、選擇性的 20-HETE 合成酶抑制劑，對重 組 CYP4A1、CYP4A2 和 CYP4A3 催化 20-HETE合成作

3、的 IC50 值分別為 17.7 nM, 12.1 nM 和 20.6 nM。HET0016種選擇性 CYP450 抑制劑，已被證明可以抑制管成和腫瘤長 1 2。IC50 & Target 17.7 nM (CYP4A1), 12.1 nM (CYP4A2), 20.6 nM (CYP4A3) 1, CYP450 2體外研究HET0016 is a selective, non-competitive and irreversible inhibitor of CYP4A 1.HET0016 (100 M; 24 hours, 48 hours) decreases migration and

4、 invasion of breast cancer metastatic cells2.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECell Proliferation Assay 2Cell Line: MDA-MB-231 cellsConcentration: 100 MIncubation Time: 24 hours, 48 hoursResult: Decreased migration and invasion of breast cancer metastatic cells體內(nèi)研究 HET0016 (10 mg/kg/d

5、ay; i.v.; for 3 weeks) reduces tumor volume and lung metastasis in animmunocompetent breast cancer mouse model 2.HET0016 reduces the metalloproteinases levels in the lungs via PI3K/AKT pathway in mice 2.HET0016 decreases expression of pro-inflammatory and growth factors and granulocytic MDSCs popula

6、tionin lung microenvironment 2.HET0016 protects BBB dysfunction after I/R by regulating the expression of MMP-9 and tight junctionproteins 3.Animal Model: 45 weeks female Balb/c mice (16-18 g) 2Dosage: 10 mg/kg/dayAdministration: Intravenously; 5 days a week; for 3 weeks; starting from day 15 of tum

7、or implantationResult: Reduced tumor volume and lung metastasis.REFERENCES1. Seki T, et al. Cytochrome P450 4A isoform inhibitory profile of N-hydroxy-N-(4-butyl-2-methylphenyl)-formamidine (HET0016), aselective inhibitor of 20-HETE synthesis. Biol Pharm Bull. 2005 Sep;28(9):1651-4.2. Borin TF, et a

8、l. HET0016 decreases lung metastasis from breast cancer in immune-competent mouse model. PLoS One. 2017 Jun13;12(6):e0178830.3. Liu Y, et al. The protective effect of HET0016 on brain edema and blood-brain barrier dysfunction after cerebral ischemia/reperfusion.Brain Res. 2014 Jan 28;1544:45-53.McePdfHeightCaution: Product has not been fully validated for medical applications