HET0016

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

HET0016 是一种高效、选择性的 20-HETE 合成酶抑制剂，对重组 CYP4A1、CYP4A2 和 CYP4A3 催化 20-HETE 合成作用的 IC50 值分别为 17.7 nM, 12.1 nM 和 20.6 nM。HET0016 是一种选择性 CYP450 抑制剂，已被证明可以抑制血管生成和肿瘤生长。

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.

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 .Cell Proliferation Assay Cell Line:MDA-MB-231 cells Concentration:100 μM Incubation Time:24 hours, 48 hours Result:Decreased migration and invasion of breast cancer metastatic cells

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.

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Others

Other Targets

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339068-25-6

206.28

C12H18N2O

>98% (HPLC)

In Vitro:?DCM 中的溶解度 : 12.5 mg/mL (60.60 mM; 超声助溶) DMSO 中的溶解度 : 5 mg/mL (24.24 mM; 超声助溶 )

CCCCc1ccc(N=CNO)c(C)c1

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(-20℃)

With Ice Pack

≥ 2 years