Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Clobenpropit dihydrobromide 是一种组胺H3R 拮抗剂/反向激动剂。它与 5-HT3 受体和 α2A/α2C 肾上腺素受体结合,对组胺H4受体起部分激动剂的作用,还能促进凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 289 | 现货 | ||
5 mg | ¥ 787 | 现货 | ||
10 mg | ¥ 1,280 | 现货 | ||
25 mg | ¥ 2,650 | 现货 | ||
50 mg | ¥ 4,230 | 现货 | ||
100 mg | ¥ 5,910 | 现货 |
产品描述 | Clobenpropit dihydrobromide is a potent antagonist and inverse agonist of histamine H3R (histamine H3LR,pEC50 of 8.07) |
靶点活性 | H2 receptor:5.6 (pKi), H3LR (human):9.44 (pKi), H4 receptor:13 nM (Ki), H3LR (rat):9.75 (pKi) |
体外活性 | Clobenpropit inhibited cell migration and increased apoptosis of pancreatic cancer cells in combination with gemcitabine.?Clobenpropit up-regulated E-cadherin, but down-regulated vimentin and matrix metalloproteinase 9 in real-time polymerase chain reaction[1]. |
体内活性 | Clobenpropit inhibited tumor growth (gemcitabine 294 46 mg vs combination 154 54 mg, P = 0.02) and enhanced apoptosis in combination with gemcitabine (control 2.5%, gemcitabine 25.8%, clobenpropit 9.7% and combination 40.9%, P = 0.001) by up-regulation of E-cadherin and down-regulation of Zeb1 in Panc-1 xenograft mouse. |
细胞实验 | Pancreatic cancer cells (Panc-1, MiaPaCa-2 and AsPC-1).Concentration: 50 Μm |
分子量 | 470.7 |
分子式 | C14H19Br2ClN4S |
CAS No. | 145231-35-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4.71 mg/mL (10 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1245 mL | 10.6225 mL | 21.245 mL | 53.1124 mL |
5 mM | 0.4249 mL | 2.1245 mL | 4.249 mL | 10.6225 mL | |
10 mM | 0.2124 mL | 1.0622 mL | 2.1245 mL | 5.3112 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。
Clobenpropit dihydrobromide 145231-35-2 Apoptosis GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor inhibit Clobenpropit histamine H3R antagonist inverse Inhibitor pancreatic agonist cancer H3LR Clobenpropit Dihydrobromide inhibitor