store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
IBMX (Methylisobutylxanthine) 是一种广谱的磷酸二酯酶 (PDE) 抑制剂,对 PDE3、PDE4 和 PDE5 均有抑制活性 (IC50=6.5/26.3/31.7 μM)。IBMX 可以增强细胞内 cAMP 水平。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 145 | 现货 | ||
10 mg | ¥ 192 | 现货 | ||
25 mg | ¥ 293 | 现货 | ||
50 mg | ¥ 415 | 现货 | ||
100 mg | ¥ 631 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 279 | 现货 |
产品描述 | IBMX (Methylisobutylxanthine) is a broad-spectrum phosphodiesterase (PDE) inhibitor with inhibitory activity against PDE3, PDE4, and PDE5 (IC50=6.5/26.3/31.7 μM). IBMX enhances the intracellular cAMP level. |
靶点活性 | PDE3:6.5 μM, PDE5:31.7 μM, PDE4:26.3 μM |
体外活性 |
方法:从 HK 喂养的大鼠分离的 CCD 用 IBMX (100 μM) 预处理 20 min,并检查 ANG II 或 cGMP 对通道活性的影响。 结果:IBMX 激活了 ROMK 通道并阻止了 ANG II 进一步激活通道。[1] 方法:豚鼠 TSMC 的原代培养物,在 IBMX (100 μM) 存在的情况下,检测 KMUP-1 对 cAMP 和 cGMP 水平的影响。 结果:IBMX 和 KMUP-1 显著增加了 cAMP 和 cGMP 水平。单独使用 KMUP-1 对 cAMP 和 cGMP 水平与在有 IBMX 的条件下没有显著差异。[2] 方法:哺乳动物细胞 CHO 用 IBMX (10-1000 μM) 处理,使用膜片钳技术测量全细胞电流。 结果:IBMX 对 THIK-1 电流影响的稳态剂量反应曲线可以拟合为 Hill 系数为 1 和 IC50 为 120 μM。[3] |
体内活性 |
方法:为检测对小鼠的代谢作用,将 IBMX (1 mg/kg) 皮下注射给小鼠,每天两次,持续七天。 结果:IBMX 显著增加了小鼠的血糖水平(血糖,mg/dl,对照=141,IBMX=210)。[4] 方法:为检测对高血糖小鼠的代谢作用,将葡萄糖 (0.5 g/kg) 和 IBMX (1 mg/kg) 股静脉注射给 Wistar 大鼠。 结果:在高血糖大鼠中,IBMX 能降低血糖,IBMX 不会改变血浆胰岛素水平,IBMX 降低了肝糖原储存。[4] |
细胞实验 | Intracellular cyclic GMP and cyclic AMP concentrations in guinea-pig TSMCs were assayed as previously described. In brief, cells were grown in 24-well plates 10^5 cells per well. At confluence, monolayer cells were washed with phosphate buffer solution (PBS) and then incubated with KMUP-1 (0.1–100 μM) in the presence of 100 μM IBMX for 20 min. Incubation was terminated by the addition of 10% trichloroacetic acid (TCA). Cell suspensions were sonicated and then centrifuged at 2500 × g for 15 min at 4°C. To remove TCA, the supernatants were extracted three times with 5 volumes of water-saturated diethyl ether. Then, the supernatants were lyophilized and the cyclic GMP or AMP of each sample was determined by using commercially available radioimmunoassay kits [1]. |
动物实验 | Male mice (25-35 g), obtained from the animal house of Faculty of Medicine, were kept in controlled environmental conditions (temperature: 23±2 oC; light-dark cycle: 7 a.m. to 7 p.m.) and were divided randomly into groups of seven. All test compounds were dissolved in DMSO and diluted to desired concentration with less than 1% DMSO. For the experiment, the test compound (IBMX, milrinone, MCPIP, mc1, mc2, mc5 or mc6) or solvent (control) was injected subcutaneously to mice at 1 mg/kg dosage twice a day (8:00 a.m. and 8:00 p.m.) for 7 days. On day 8, animals were anesthetized with intraperitoneal injection of thiopental (80 mg/kg) and blood samples were obtained from their hearts and then the liver was dissected. Each sample was centrifuged for 5 min and its serum was separated [3]. |
别名 | IBMX,3-异丁基-1-甲基黄嘌呤, 3-Isobutyl-1-methylxanthine, 1-Methyl-3-Isobutylxanthine, Methylisobutylxanthine, Isobutylmethylxanthine |
化合物与蛋白结合的复合物 |
Crystal structure of PDE8A catalytic domain in complex with IBMX |
分子量 | 222.24 |
分子式 | C10H14N4O2 |
CAS No. | 28822-58-4 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 2.22mg/mL (10mM), Sonication is recommended.
DMSO: 16.7 mg/mL(75 mM)
Ethanol: 22.24mg/mL (100mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO / Ethanol | 1 mM | 4.4996 mL | 22.4982 mL | 44.9964 mL | 112.491 mL |
5 mM | 0.8999 mL | 4.4996 mL | 8.9993 mL | 22.4982 mL | |
10 mM | 0.45 mL | 2.2498 mL | 4.4996 mL | 11.2491 mL | |
DMSO / Ethanol | 20 mM | 0.225 mL | 1.1249 mL | 2.2498 mL | 5.6246 mL |
50 mM | 0.09 mL | 0.45 mL | 0.8999 mL | 2.2498 mL | |
Ethanol | 100 mM | 0.045 mL | 0.225 mL | 0.45 mL | 1.1249 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。
IBMX 28822-58-4 Metabolism PDE IBMX,3-异丁基-1-甲基黄嘌呤 Phosphodiesterase (PDE) 3-Isobutyl-1-methylxanthine 1-Methyl-3-Isobutylxanthine inhibit Inhibitor Methylisobutylxanthine Isobutylmethylxanthine inhibitor