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同义名 : | - |
CAS号 : | 99420-15-2 | |
货号 : | A738642 | |
分子式 : | C13H8N2OS | |
纯度 : | 97% | |
分子量 : | 240.28 | |
MDL号 : | MFCD19690951 | |
存储条件: |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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溶解度 : | - | |
动物实验配方: |
生物活性 | |||
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描述 | Macrophage migration inhibitory factor (MIF) is a ubiquitous protein released by ischemic heart tissue and has been shown to activate the AMP-activated protein kinase pathway. BTZO-1 is a 1,3-benzothiazin-4-one derivative that activates antioxidant response element (ARE)-mediated gene expression and suppresses oxidative stress-induced cardiomyocyte apoptosis in vitro. It binds to MIF with a Kd value of 68.6nM. BTZO-1 at 0.37μM suppressed the internucleosomal cleavage of genomic DNA and doxorubicin-induced cell death in cardiomyocytes culturing in serum-free medium. In H9c2 cells transfected with pGL3-ARE-Luc, treatment with BTZO-1 (0 to 10μM) led to a dose-dependent increase in luciferase activities. The MEC2.0 of BTZO-1 for ARE activation was 0.82μM. BTZO-1 at 40 and 400nM also increased protein levels of GST Ya and HO-1 in cardiomyocytes. The upregulated mRNA expressions of GST Ya and HO-1 by 3 μM BTZO-1 was decreased in MIF-reduced H9c2 cells. BTZO-2, an active BTZO-1 derivative, reduced infarct size caused by myocardial ischemia/reperfusion in rats at a dosage of 10mg/kg[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.16mL 0.83mL 0.42mL |
20.81mL 4.16mL 2.08mL |
41.62mL 8.32mL 4.16mL |
参考文献 |
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