Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GIBH130 是一种有效的神经炎症抑制剂,可作用于活化的小胶质细胞,明显抑制IL-1β的分泌(IC50:3.4 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 395 | 现货 | ||
2 mg | ¥ 568 | 现货 | ||
5 mg | ¥ 913 | 现货 | ||
10 mg | ¥ 1,580 | 现货 | ||
25 mg | ¥ 3,490 | 现货 | ||
50 mg | ¥ 4,970 | 现货 | ||
100 mg | ¥ 7,230 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 996 | 现货 |
产品描述 | GIBH-130 markedly inhibits the IL-1β secretion by activated microglia (IC50: 3.4 nM). GIBH-130 is an effective inhibitor of neuroinflammation. |
靶点活性 | IL-1β:3.4 nM, NO:46.24 μM, TNF-α:40.82 μM |
体外活性 | GIBH-130 is a novel anti-neuroinflammatory agent that is identified through microglia-based phenotypic screenings. GIBH-130 (IC50 3.4 nM) is identified in screenings as one of the most effective inhibitors with an acceptable half-life. Pretreatment of microglia with GIBH-130 significantly reduces the production of these factors in response to Lipopolysaccharides (LPS) stimulation, and the extent of the reduction is dependent on the concentrations of GIBH-130. GIBH-130 has weak inhibition for NO (IC50: 46.24 μM) and TNF-α (IC50: 40.82 μM). Notably, pretreatment with GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50: 3.4 nM). The inhibitory efficiency of GIBH-130 (20 nM) is comparable to 20 μM minocycline against IL-1β release. IL-1β is one of the major cytokines during the neuroinflammatory progression of the AD [1]. |
体内活性 | In both β amyloid-induced and APP/PS1 double transgenic Alzheimer's murine models, GIBH-130 (0.25 mg/kg) has comparable in vivo efficacy of cognitive impairment relief to donepezil and memantine respectively. As a potential drug candidate targeting in CNS, GIBH-130 is found to be orally bioavailable in rats, with 74.91% bioavailability and 4.32 h half-life. In addition, GIBH-130 displays good penetration ability across blood-brain barrier (AUCBrain/Plasma=0.21)[1]. |
分子量 | 360.41 |
分子式 | C20H20N6O |
CAS No. | 1252608-59-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
DMSO: 27.5 mg/mL (76.3 mM), Sonification is recommended
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7746 mL | 13.8731 mL | 27.7462 mL | 69.3654 mL |
5 mM | 0.5549 mL | 2.7746 mL | 5.5492 mL | 13.8731 mL | |
10 mM | 0.2775 mL | 1.3873 mL | 2.7746 mL | 6.9365 mL | |
20 mM | 0.1387 mL | 0.6937 mL | 1.3873 mL | 3.4683 mL | |
50 mM | 0.0555 mL | 0.2775 mL | 0.5549 mL | 1.3873 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。
GIBH-130 1252608-59-5 Apoptosis Immunology/Inflammation IL Receptor TNF Interleukin Inhibitor Interleukin Related GIBH 130 inhibit GIBH130 inhibitor