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IBMX

IBMX

产品编号 T1713   CAS 28822-58-4
别名: IBMX,3-异丁基-1-甲基黄嘌呤, 3-Isobutyl-1-methylxanthine, 1-Methyl-3-Isobutylxanthine, Methylisobutylxanthine, Isobutylmethylxanthine

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。

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IBMX Chemical Structure
IBMX, CAS 28822-58-4
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: IBMX (T1713)
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纯度: 100%
纯度: 100%
纯度: 99.86%
纯度: 99.81%
纯度: 99.8%
纯度: 99.80%
纯度: 99.76%
纯度: 99.03%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

T1713_2

Crystal structure of PDE8A catalytic domain in complex with IBMX

分子量 222.24
分子式 C10H14N4O2
CAS No. 28822-58-4

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 2.22mg/mL (10mM), Sonication is recommended.

DMSO: 16.7 mg/mL(75 mM)

Ethanol: 22.24mg/mL (100mM), Sonication is recommended.

溶液配制表

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

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TargetMol Library Books参考文献

1. Wei Y, et al. Angiotensin II type 2 receptor regulates ROMK-like K⁺ channel activity in the renal cortical collecting duct during high dietary K⁺ adaptation. Am J Physiol Renal Physiol. 2014 Oct 1;307(7):F833-43. 2. Wu BN, et al. KMUP-1, a xanthine derivative, induces relaxation of guinea-pig isolated trachea: the role of the epithelium, cyclic nucleotides and K+ channels. Br J Pharmacol. 2004 Aug;142(7):1105-14. 3. Zou X, et al. The Phosphodiesterase Inhibitor IBMX Blocks the Potassium Channel THIK-1 from the Extracellular Side. Mol Pharmacol. 2020 Aug;98(2):143-155. 4. Cadamuro M, et al. Low-Dose Paclitaxel Reduces S100A4 Nuclear Import to Inhibit Invasion and Hematogenous Metastasis of Cholangiocarcinoma. Cancer Res. 2016 Aug 15;76(16):4775-84. 5. Sun C, Li X, Guo E, et al. MCP-1/CCR-2 axis in adipocytes and cancer cell respectively facilitates ovarian cancer peritoneal metastasis[J]. Oncogene. 2019: 1-15. 6. Xiaoli F, Yaqing Z, Ruhui L, et al. Graphene oxide disrupted mitochondrial homeostasis through inducing intracellular redox deviation and autophagy-lysosomal network dysfunction in SH-SY5Y cells[J]. Journal of Hazardous Materials. 2021: 126158.

TargetMol Library Books文献引用

1. Yan Z, Ruan B, Wang S, et al.RNA-binding Protein QKI Inhibits Osteogenic Differentiation Via Suppressing Wnt Pathway.Archives of Medical Research.2023: 102853. 2. Chen S, Zhou X, Li W, et al.Development of a novel peptide targeting GPR81 to suppress adipocyte-mediated tumor progression.Biochemical Pharmacology.2023: 115800. 3. Lin S, Zhong L, Chen J, et al.GDF11 inhibits adipogenesis of human adipose-derived stromal cells through ALK5/KLF15/β-catenin/PPARγ cascade.Heliyon.2023: e13088. 4. Sun C, Li X, Guo E, et al. MCP-1/CCR-2 axis in adipocytes and cancer cell respectively facilitates ovarian cancer peritoneal metastasis. Oncogene. 2019: 1-15. 5. Xiaoli F, Yaqing Z, Ruhui L, et al. Graphene oxide disrupted mitochondrial homeostasis through inducing intracellular redox deviation and autophagy-lysosomal network dysfunction in SH-SY5Y cells. Journal of Hazardous Materials. 2021: 126158.
CP671305 GSK256066 Trifluoroacetate Vardenafil hydrochloride trihydrate Triflusal Levosimendan Verofylline Choline theophyllinate Udenafil

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 抑制剂库 已知活性化合物库 活性脂质化合物库 抗心血管疾病化合物库 铜死亡化合物库 抗阿尔茨海默症化合物库 NO PAINS 化合物库 经典已知活性库 免疫/炎症分子化合物库

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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。

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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。

Keywords

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

 

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