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BTZO-1

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Chemical Structure| 99420-15-2 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：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 7 mg/mL(29.13 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
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
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

[1]Kimura H, Sato Y, Tajima Y, et al. BTZO-1, a cardioprotective agent, reveals that macrophage migration inhibitory factor regulates ARE-mediated gene expression. Chem Biol. 2010;17(12):1282-1294. doi:10.1016/j.chembiol.2010.10.011