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114432-13-2

中文名稱 泛托法隆
英文名稱 Fantofarone
CAS 114432-13-2
分子式 C31H38N2O5S
分子量 550.71
MOL 文件 114432-13-2.mol
更新日期 2023/10/17 22:29:14
114432-13-2 結(jié)構(gòu)式 114432-13-2 結(jié)構(gòu)式

基本信息

中文別名
泛托法隆
3,4-二甲氧基-N-甲基-N- [3-[4-[[2-(1-甲基乙基)-1-氮茚基]磺?;鵠苯氧基]丙基]苯乙胺
英文別名
CS-2766
SR-33557
Fantofarone
FANTOFARONE
SR-33557
SR33557
114432-13-2
2-Isopropyl-1-[[4-[3-[[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino]propoxy]phenyl]sulfonyl]indolizine
3,4-Dimethoxy-N-methyl-N-[3-[4-[[2-(1-methylethyl)-1-indolizinyl]sulfonyl]phenoxy]propyl]benzeneethanamine
Benzeneethanamine, 3,4-dimethoxy-N-methyl-N-[3-[4-[[2-(1-methylethyl)-1-indolizinyl]sulfonyl]phenoxy]propyl]-

物理化學(xué)性質(zhì)

熔點82-83°
密度dz 1.21 g/cm3
儲存條件-20°C儲存
溶解度DMF: 10 mg/ml; DMSO: 10 mg/ml
酸度系數(shù)(pKa)8.34 ± 0.05(at 25℃)
形態(tài)結(jié)晶固體
顏色Light yellow to yellow

常見問題列表

生物活性
Fantofarone 是鈣離子通道 (Calcium Channel) 的強效拮抗劑。
靶點

Calcium Channel.

體外研究

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. Furthermore, when used at similar subinhibitory fractions of their IC 50 , VR is 2 to 3 times more potent than Fantofarone in decreasing CQ resistance.

體內(nèi)研究

Treatment with isosorbide dinitrate (0.3 mg/kg, i.v.) or Fantofarone (50 mg/kg, i.v.), a reduction is observed in the occurrence and severity of vasospasm, 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.

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