99420-15-2|2-(Pyridin-2-yl)-4H-benzo[e][1,3]thiazin-4-one|CsnPharm

CAS No.: 99420-15-2

BTZO-1 Catalog No. CSN22727

Synonyms: 2-(Pyridin-2-yl)-4H-benzo[e][1,3]thiazin-4-one

BTZO 1 is a macrophage migration inhibitory factor (MIF) binder with Kd of 68.6 nM.

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实验方案

技术信息

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 K_d 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 MEC_2.0 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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.1618 mL
- 20.8090 mL
- 41.6180 mL
- 5 mM
- 0.8324 mL
- 4.1618 mL
- 8.3236 mL
- 10 mM
- 0.4162 mL
- 2.0809 mL
- 4.1618 mL

技术信息

CAS号

99420-15-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H8N2OS

运输

蓝冰

分子量

240.28

别名

2-(Pyridin-2-yl)-4H-benzo[e][1,3]thiazin-4-one

溶解度

DMSO	10.0 mg/mL (41.6 mM)
Water	Insoluble
Ethanol	4.0 mg/mL (16.6 mM)

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