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HET0016 is a potent and selective 20-HETE synthase inhibitor (IC50s: 17.7 nM, 12.1 nM, and 20.6 nM for recombinant CYP4A1-, CYP4A2-, and CYP4A3-catalyzed 20-HETE synthesis) and a selective CYP450 inhibitor, shown to inhibit angiogenesis and tumor growth.
HET0016 is a potent and selective 20-HETE synthase inhibitor (IC50s: 17.7 nM, 12.1 nM, and 20.6 nM for recombinant CYP4A1-, CYP4A2-, and CYP4A3-catalyzed 20-HETE synthesis) and a selective CYP450 inhibitor, shown to inhibit angiogenesis and tumor growth.
规格 | 价格 | 库存 | 数量 |
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1 mg | ¥ 183 | 现货 | |
5 mg | 询价 | 现货 |
产品描述 | HET0016 is a potent and selective 20-HETE synthase inhibitor (IC50s: 17.7 nM, 12.1 nM, and 20.6 nM for recombinant CYP4A1-, CYP4A2-, and CYP4A3-catalyzed 20-HETE synthesis) and a selective CYP450 inhibitor, shown to inhibit angiogenesis and tumor growth. |
靶点活性 | CYP4A1:17.7 nM , CYP4A2: 12.1 nM , CYP4A3: 20.6 nM |
体外活性 | HET0016 (100 μM; 24 hours, 48 hours) decreases migration and invasion of breast cancer metastatic cells .HET0016 is a selective, non-competitive and irreversible inhibitor of CYP4A . |
体内活性 | 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.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. |
分子量 | 206.28 |
分子式 | C12H18N2O |
CAS No. | 339068-25-6 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DCM: 12.5 mg/mL (60.60 mM), Sonication is recommended. DMSO: 5 mg/mL (24.24 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO/DCM
DCM
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