泛托法隆 T4669

Product Introduction
Bioactivity


英文名: Fantofarone

描述: Fantofarone (SR 33557) 是一种钙离子通道的强效拮抗剂。

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.

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 150 mg/mL (272.38 mM)


关键字: Parasite | Fantofarone | Ca channels | Calcium Channel | SR33557 | inhibit | SR-33557 | Inhibitor | Ca2+ channels

相关产品: NPS-2143 | Crobenetine | Catharanthine | Ziconotide Acetate (107452-89-1 free base) | Cav 3.2 inhibitor 4 | Lercanidipine | (R)-(+)-Bay-K-8644 | Efonidipine | Felodipine | Maurocalcine

相关库: Ion Channel Inhibitor Library | Anti-Cancer Compound Library | Calcium Channel Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | Inhibitor Library | Anti-Parasitic Compound Library | Bioactive Compound Library | Anti-Infection Compound Library

泛托法隆 T4669信息由TargetMol中国为您提供，如您想了解更多关于泛托法隆 T4669报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途