Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Cinobufotalin 是一种从蟾蜍的皮肤分泌物中提取的强心类固醇或丁二烯内酯。它已被用作强心药,利尿药和止血药,也是潜在的抗肺癌药物。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 348 | 现货 | ||
2 mg | ¥ 498 | 现货 | ||
5 mg | ¥ 728 | 现货 | ||
10 mg | ¥ 1,220 | 现货 | ||
25 mg | ¥ 2,080 | 现货 | ||
50 mg | ¥ 3,130 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 753 | 现货 |
产品描述 | Cinobufotalin is a main cardiac toxin in toad, it is a novel anti-HCC agent, it induces growth inhibition and apoptosis in cultured HCC cells through ceramide production. Cinobufotalin is also an effective reversal agent for the multidrug resistance of tumors, it can reverse the adriamycin-resistance in Raji/ADR cells and the expression of P-gp and MRP-1 proteins. Cinobufotalin can promote the dendritic cells(DCs) derived from peripheral blood of patients with chronic hepatitis B to mature and effectively enhance its(the DCs') capabilities, therefore the treatment of cinobufotalin may potentiate the antiviral immunity of the patients with chronic hepatitis B(CHB). |
体外活性 | Hepatocellular carcinoma (HCC) is a highly aggressive and lethal neoplasm with poor prognosis. The aim of this study is to investigate the anticancer activity of Cinobufotalin, a bufadienolide isolated from toad venom, in cultured HCC cells, and to study the underlying mechanisms. METHODS AND RESULTS:We found that Cinobufotalin (at nmol/L) significantly inhibited HCC cell growth and survival while inducing considerable cell apoptosis. Further, Cinobufotalin inhibited sphingosine kinase 1 (SphK1) activity and induced pro-apoptotic ceramide production. Ceramide synthase-1 small hairpin RNA (shRNA)-depletion inhibited Cinobufotalin-induced ceramide production and HCC cell apoptosis. On the other hand, the glucosylceramide synthase (GCS) inhibitor 1-phenyl-2-decanoylamino-3-morpholino-1-propanol (PDMP) facilitated Cinobufotalin-induced ceramide production and cell apoptosis. SphK1 inhibitor II (SKI-II), similar to Cinobufotalin, increased cellular ceramide level and promoted HCC cell apoptosis. Finally, we observed that Cinobufotalin inactivated Akt-S6K1 signaling in HepG2 cells, which was again inhibited by ceramide synthase-1 shRNA-depletion. CONCLUSIONS:In conclusion, the results of this study suggest that Cinobufotalin induces growth inhibition and apoptosis in cultured HCC cells through ceramide production. Cinobufotalin may be investigated as a novel anti-HCC agent. |
别名 | 华蟾毒它灵, 华蟾素 |
分子量 | 458.54 |
分子式 | C26H34O7 |
CAS No. | 1108-68-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (89.82 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 | 2.1808 mL | 10.9042 mL | 21.8083 mL | 54.5209 mL |
5 mM | 0.4362 mL | 2.1808 mL | 4.3617 mL | 10.9042 mL | |
10 mM | 0.2181 mL | 1.0904 mL | 2.1808 mL | 5.4521 mL | |
20 mM | 0.109 mL | 0.5452 mL | 1.0904 mL | 2.726 mL | |
50 mM | 0.0436 mL | 0.2181 mL | 0.4362 mL | 1.0904 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。
Cinobufotalin 1108-68-5 Cytoskeletal Signaling Immunology/Inflammation Membrane transporter/Ion channel Neuroscience PI3K/Akt/mTOR signaling IL Receptor P-gp Akt MRP inhibit 华蟾毒它灵 Inhibitor 华蟾素 inhibitor