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化學(xué)性質(zhì):
規(guī)格 | 10mg 50mg |
CAS | 99420-15-2 |
別名 |
|
化學(xué)名 | 2-(pyridin-2-yl)-4H-benzo[e][1,3]thiazin-4-one |
分子式 | C13H8N2OS |
分子量 | 240.28 |
溶解度 | <4.81mg/ml in DMSO |
儲存條件 | Store at RT |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產(chǎn)品描述:
MIF is a ubiquitous protein. It is a specific BTZO 1-binding protein. MIF is released by ischemic heart tissue. It activates the cardioprotective AMP-activated protein kinase (AMPK) pathway. MIF was reported to be a key upstream regulator of the innate and acquired immune response. MIF regulates cytokine secretion, counter-regulates glucocorticoids in inflammation, inhibits oxidative stress-induced cell death, and activates components of the Jun-activation domain-binding protein-1 (Jab-1) pathway and mitogen-activated protein kinase [1].
H9c2 cells transfected by pGL3-ARE-Luc were treated with rMIF in the presence of BTZO 1 at 1 μM. In this system, dose-dependently induced luciferase activity was found. When transfected cells were treated with rMIF alone, ARE-mediated luciferase activity was scarcely induced. Treatment with BTZO 1, also promoted rMIF induction of HO-1 mRNA and GST Ya in H9c2 cells. In H9c2 cells, pretreatment with BTZO 1 at 30 μM caused an approximately 20% decrease in tautomerase activity (measured in the cell lysate). This suggested that there was a direct interaction between MIF and BTZO 1 in H9c2 cells [1].
BTZO 2 is a BTZO 1 analog with a better ADME profile. 24 hr after reperfusion with drug, mean values for the area at risk were 46% ± 3% and 48% ± 2% for vehicle and BTZO 2, respectively. In control rats, left anterior descending coronary artery (LAD) occlusion and reperfusion caused an infarct size of 43% of the area at risk. Compared to control, intraperitoneal administration with BTZO 2 at 10 mg/kg 1 hr prior to LAD occlusion and 2 and 8 hr after reperfusion caused an approximately 45% reduction in the infarct size [1].
Reference:
[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. Chemistry & biology, 2010, 17(12): 1282-1294.
特別提醒:
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原創(chuàng)作者:上海莼試生物技術(shù)有限公司
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