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Fantofarone (SR 33557) 是一种钙离子通道的强效拮抗剂。
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Fantofarone (SR 33557) 是一种钙离子通道的强效拮抗剂。
规格 | 价格 | 库存 | 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 x 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 | 从所述内容可以看出,钙通道阻滞剂VIZ和Fantofarone(SR)与CQ相比具有较弱的内在抗疟疾特性,且在对抗CQ抵抗性寄生虫上比对抗CQ敏感性寄生虫略显更有效。值得注意的是,Fantofarone的效力大约是verapamil的10倍。Fantofarone(SR)对两种P. fdciparum菌株的效力是苯基烷胺类verapamil(VR)的10倍。根据同位图分析显示,这两种钙通道阻滞剂能增强对CQ抵抗性P. fufcipurum菌株的CQ敏感性活动,其中verapamil的效力比Fantofarone高出2到3倍。此外,在使用类似其IC50的亚抑制份额时,VR在降低CQ抗药性方面的效力比Fantofarone高出2到3倍。 |
体内活性 | 在使用异硝酸异山梨酯(0.3 mg/kg,静脉注射)或Fantofarone(50 mg/kg,静脉注射)时,观察到血管痉挛发生率和严重度的降低,而verapamil(0.2 mg/kg,静脉注射)的效果则明显较弱。尽管异硝酸异山梨酯能完全抑制远端AIV,但对近端直径减少没有显著影响。在抑制远端和近端血管痉挛方面,有效的化合物是Fantofarone,它在整个实验中显著减少了AIV。相比之下,Verapamil未能显著减少AIV。 |
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 | 泛托法隆, SR 33557 |
分子量 | 550.71 |
分子式 | C31H38N2O5S |
CAS No. | 114432-13-2 |
Smiles | COc1ccc(CCN(C)CCCOc2ccc(cc2)S(=O)(=O)c2c(cn3ccccc23)C(C)C)cc1OC |
密度 | 1.16g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 150 mg/mL (272.38 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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