Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fantofarone (SR 33557) 是一种钙离子通道的强效拮抗剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 328 | 现货 | ||
5 mg | ¥ 745 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,480 | 现货 | ||
50 mg | ¥ 4,130 | 现货 | ||
100 mg | ¥ 5,390 | 现货 | ||
500 mg | ¥ 10,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,320 | 现货 |
产品描述 | Fantofarone (SR 33557) is a highly potent antagonist of Calcium Channel. |
体外活性 | It can be seen that the calcium channel blockers VIZ and Fantofarone (SR) possess a weak intrinsic antimalarial property compared to CQ, and both appear slightly more potent on the CQ-resistant than on the CQ-sensitive parasites. Interestingly, Fantofarone is ca. 10 times more potent than verapamil. Fantofarone (SR) is 10 times more potent than the phenylalkylamine verapamil (VR) on the two P. fdciparum strains. As revealed by the isobolograms, the two calcium channel blockers potentiate the CQ sensitivity activity on the CQ-resistant P. fufcipurum strain, verapamil appearing 2 to 3 times more potent than Fantofarone. Moreover, VR is 2 to 3 times more potent than Fantofarone in decreasing CQ resistance when used at similar subinhibitory fractions of their IC50. |
体内活性 | A reduction is observed in the occurrence and severity of vasospasm with isosorbide dinitrate (0.3 mg/kg, i.v.) or Fantofarone (50 mg/kg, i.v.), whereas verapamil (0.2 mg/kg, i.v.) is much less effective. Although it totally inhibits distal AIV, isosorbide dinitrate does not significantly affect proximal diameter decrease. The most potent compound with regard to both the distal and proximal vasospasms is Fantofarone, which significantly reduces AIV throughout the experiment. Verapamil does not reduce AIV significantly. |
动物实验 | Male White rabbits are used in this study (3.0-3.2 kg). All surgical procedures are performed under anaesthesia with a mixture of ketamine and xylazine. At the end of the experiments, the animals are sacrificed by a pentobarbital overdose. The proximal femoral arteries are exposed, and the isolated arterial segments are desiccated by air infusion delivered at a rate of 80 mL/min for 8 min. After desiccation is completed, the ligatures are released and flow is restored. At the day of surgery, a 2% cholesterol/6% peanut oil diet is started for 2 weeks. Before angioplasty, the animals are randomized in 4 groups of 10 animals:1. Placebo, 1 mL/kg of NaCl 0.9%, 2. Isosorbide dinitrate, 0.3 mg/kg, 3. Verapamil, 0.2 mg/kg, 4. Fantofarone, 50 mg/kg. The doses of isosorbide dinitrate, verapamil, and fantofarone are defined in a pilot experiment as the highest doses which did not show any hypotensive effect per se and are chosen very carefully according to their activity measured in other pharmacological models. |
别名 | SR 33557, 泛托法隆 |
分子量 | 550.71 |
分子式 | C31H38N2O5S |
CAS No. | 114432-13-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 150 mg/mL (272.38 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 | 1.8158 mL | 9.0792 mL | 18.1584 mL | 45.3959 mL |
5 mM | 0.3632 mL | 1.8158 mL | 3.6317 mL | 9.0792 mL | |
10 mM | 0.1816 mL | 0.9079 mL | 1.8158 mL | 4.5396 mL | |
20 mM | 0.0908 mL | 0.454 mL | 0.9079 mL | 2.2698 mL | |
50 mM | 0.0363 mL | 0.1816 mL | 0.3632 mL | 0.9079 mL | |
100 mM | 0.0182 mL | 0.0908 mL | 0.1816 mL | 0.454 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。
Fantofarone 114432-13-2 Membrane transporter/Ion channel Metabolism Microbiology/Virology Parasite Calcium Channel SR 33557 泛托法隆 Ca channels SR33557 inhibit SR-33557 Inhibitor Ca2+ channels inhibitor