Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Cafestol 是咖啡特有的一种二萜,可靶向 AP-1 抑制ERK,有化学预防、抗肿瘤、保肝、抗氧化和抗炎作用。它通过抑制NF-kB 活化途径强烈的抑制 PGE2的产生,还抑制 LGE 激活的 RAW264.7 细胞中的PGE2产生和环氧合酶(COX-2)的 mRNA 表达。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 263 | 现货 | ||
5 mg | ¥ 579 | 现货 | ||
10 mg | ¥ 928 | 现货 | ||
25 mg | ¥ 1,680 | 现货 | ||
50 mg | ¥ 2,480 | 现货 | ||
100 mg | ¥ 3,690 | 现货 |
产品描述 | CAFESTOL is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. |
体外活性 | The precise molecular mechanism of the antiinflammatory activity of cafestol in terms of prostaglandin E(2) (PGE(2)) production, a critical factor involved in inflammatory responses. Cafestol inhibited both PGE(2) production and the mRNA expression of cyclooxygenase (COX)-2 from lipopolysaccharide (LPS)-treated RAW264.7 cells. This compound strongly decreased the translocation of c-Jun into the nucleus and AP-1 mediated luciferase activity. In kinase assays using purified extracellular signal-regulated kinase 2 (ERK2) or immunoprecipitated ERK prepared from LPS-treated cells in the presence or absence of cafestol, it was found that this compound can act as an inhibitor of ERK2 but not of ERK1 and mitogen-activated protein kinase kinase 1 (MEK 1). Suggest that cafestol may be a novel ERK inhibitor with AP-1-targeted inhibitory activity against PGE(2) production in LPS-activated RAW264.7 cells[1]. |
体内活性 | CAFESTOL possesses antidiabetic properties in KKAy mice. Consequently, cafestol may contribute to the reduced risk of developing T2D in coffee consumers and has a potential role as an antidiabetic drug[2]. |
动物实验 | Cafestol can postpone development of T2D in KKAy mice. Forty-seven male KKAy mice were randomized to consume chow supplemented daily with either 1.1 (high), 0.4 (low), or 0 (control) mg of cafestol for 10 weeks. Collected blood samples for fasting glucose, glucagon, and insulin as well as liver, muscle, and fat tissues for gene expression analysis. Isolated islets of Langerhans and measured insulin secretory capacity. After 10 weeks of intervention, fasting plasma glucose was 28-30% lower in cafestol groups compared with the control group (p < 0.01). Fasting glucagon was 20% lower and insulin sensitivity improved by 42% in the high-cafestol group (p < 0.05). Cafestol increased insulin secretion from isolated islets by 75-87% compared to the control group (p < 0.001)[2]. |
别名 | 咖啡醇, 咖啡油醇 |
分子量 | 316.43 |
分子式 | C20H28O3 |
CAS No. | 469-83-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5 mg/mL (15.8 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.1603 mL | 15.8013 mL | 31.6026 mL | 79.0064 mL |
5 mM | 0.6321 mL | 3.1603 mL | 6.3205 mL | 15.8013 mL | |
10 mM | 0.316 mL | 1.5801 mL | 3.1603 mL | 7.9006 mL |
中药材名称 | 中药材拉丁名 | 性 | 味 | 归经 |
苦石莲 | Caesalpinia minax Hance | 寒 | 苦 | 心, 脾, 肾 |
中成药名称 | 处方组成 | 主治疾病 | 中成药类型 |
益智温肾十味丸 | 益智,干姜,白硇砂,荜茇,榧子,莲子,苦石莲,方海,冬葵果,麝香 | 口服,一次11~15丸,一日1~2次。 | 扶正药 |
那如八味丸 | 诃子,制草乌,荜茇,芒果核,莲子,白豆蔻,苦石莲,石决明(煅) | 口服,一次9~11粒,一日1次,或遵医嘱。 | 扶正药 |
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。
CAFESTOL 469-83-0 Immunology/Inflammation MAPK Neuroscience NF-Κb ERK NF-κB COX PGE Synthase Inhibitor Nuclear factor-kappaB 咖啡醇 Cyclooxygenase PGE synthase Nuclear factor-κB Prostaglandin E synthase inhibit 咖啡油醇 Extracellular signal regulated kinases inhibitor