Powder: -20°C for 3 years | In solvent: -80°C for 1 year
3-TYP (3-(1H-1,2,3-triazol-4-yl) pyridine) 是选择性SIRT3抑制剂,IC50值为 16 nM。它对 SIRT1 和 SIRT2 的选择性强,IC50值分别为 88 和 92 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 218 | 现货 | ||
5 mg | ¥ 481 | 现货 | ||
10 mg | ¥ 823 | 现货 | ||
25 mg | ¥ 1,490 | 现货 | ||
50 mg | ¥ 2,490 | 现货 | ||
100 mg | ¥ 3,770 | 现货 | ||
500 mg | ¥ 8,380 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 481 | 现货 |
产品描述 | 3-TYP (3-(1H-1,2,3-triazol-4-yl) pyridine) is a selective SIRT3 inhibitor. |
靶点活性 | SIRT1:88 nM, SIRT3:16 nM, SIRT2:92 nM |
体外活性 | 3-TYP significantly attenuates melatonin-induced increases in deacetylated-SOD2 expression and SOD2 activity in HepG2 cells exposed to Cd. 3-TYP inhibits melatonin-enhanced SIRT3 activity while not affecting SIRT3 protein expression. 3-TYP pretreatment reverses the protective effects of melatonin on cadmium (Cd)-induced mitochondrial-derived O2•− production and autophagic cell death. |
体内活性 | 3-TYP significantly decreases SIRT3 activity and increases the acetylation of SOD2 compared with that in the control group, without influencing SIRT3 expression. 3-TYP attenuates the cardioprotective effects of melatonin by decreasing the LVEF and LVFS after 24 hours of reperfusion. 3-TYP also increases the infarct size, serum LDH levels, and apoptotic ratio compared with those in the IR+Mel group. 3-TYP (50 mg/kg, i.p.) does not markedly influence the LVEF, LVFS, infarct size, serum LDH levels, apoptosis, and oxidative stress compared with those of the Sham group. Furthermore, 3-TYP has little effect on gp91phox, Nrf2, NQO 1, Bax, Bcl-2, Caspase-3, and cleaved Caspase-3 expression levels, compared with the Sham group. |
细胞实验 | Cell viability is analyzed using Cell Counting Kit-8. 1×104 cells are inoculated into 96-well plates. After being treated, 90 μL of medium and 10 μL of CCK-8 solution are added to each well. The cells are then incubated at 37°C for 2 h. After incubation, the absorption at 450 nm is measured using an Infinite? M200 Microplate Reader. The results are expressed as a percentage of the control. The cell death is also evaluated using the trypan blue assay. HepG2 cells are plated in the 6-well plates (5×105 cells per well) and incubated for 24 h. After being treated with Cd or melatonin, the cells are detached with 300 μL trypsin-EDTA solution. The mixture of detached cells is centrifugated at 300 g for 5 min. Then, the residue is combined with 800 μL trypan blue solution and dispersed. After 3 min staining, cells are counted using an automated cell counter. The dead cells are stained with the blue color. Cell mortality (%) is expressed as percentage of the dead cell number/the total cell number. |
动物实验 | 3-TYP is formulated in 1% ethanol.Male C57BL/6 mice are anesthetized with 2% isoflurane, and myocardial ischemia is produced by temporarily exteriorizing the heart via a left thoracic incision and placing a 6-0 silk suture slipknot around the left anterior descending coronary artery. After 30 minutes of myocardial ischemia, the slipknot is released, and the myocardium is reperfused for 3 hour (for western blot analysis and oxidative stress measurement) or 24 hour (for cardiac function, apoptotic index and infarct size determination). Sham-operated mice undergo the same surgical procedures except the suture placed under the left coronary artery is not tied. Ten minutes before reperfusion, mice are randomized to receive either vehicle (1% ethanol) or melatonin (20 mg/kg) by intraperitoneal injection. C57BL/6 mice are randomly divided into the following groups: (i) Sham group: mice underwent the sham operation and are treated with vehicle (1% ethanol); (ii) Mel group: mice are treated with melatonin (20 mg/kg via intraperitoneal injection); (iii) IR+V group: mice underwent the MI/R operation and are treated with vehicle (1% ethanol); (iv) IR+Mel group: mice underwent the MI/R operation and are treated with melatonin (20 mg/kg via intraperitoneal injection 10 minutes before reperfusion); (v) IR+Mel+3-TYP group: mice are pretreated with 3-TYP (3-TYP is intraperitoneally injected at a dose of 50 mg/kg every 2 days for a total of three doses prior to the MI/R surgery), subjected to the MI/R operation, and treated with melatonin (20 mg/kg via intraperitoneal injection 10 minutes before reperfusion); and (vi) IR+3-TYP group: mice are pretreated with 3-TYP and then subjected to the MI/R operation. |
别名 | 3-(1H-1,2,3-triazol-4-yl) pyridine |
分子量 | 146.15 |
分子式 | C7H6N4 |
CAS No. | 120241-79-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 5 mg/mL (34.21 mM)
Ethanol: 28 mg/mL (191.6 mM)
DMSO: 28 mg/mL (191.6 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / Ethanol / DMSO | 1 mM | 6.8423 mL | 34.2114 mL | 68.4229 mL | 171.0571 mL |
5 mM | 1.3685 mL | 6.8423 mL | 13.6846 mL | 34.2114 mL | |
10 mM | 0.6842 mL | 3.4211 mL | 6.8423 mL | 17.1057 mL | |
20 mM | 0.3421 mL | 1.7106 mL | 3.4211 mL | 8.5529 mL | |
Ethanol / DMSO | 50 mM | 0.1368 mL | 0.6842 mL | 1.3685 mL | 3.4211 mL |
100 mM | 0.0684 mL | 0.3421 mL | 0.6842 mL | 1.7106 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
3-TYP 120241-79-4 Chromatin/Epigenetic DNA Damage/DNA Repair Sirtuin Inhibitor 3-(1H-1,2,3-triazol-4-yl) pyridine 3TYP 3 TYP inhibit inhibitor