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Ganaplacide

Ganaplacide用途

Ganaplacide(KAF156)是第一类口服活性咪唑类哌嗪抗疟药。Ganaplacide对广泛的疟原虫物种具有活性,包括抗药性寄生虫。Ganaplacide在寄生虫的无性和性血液阶段以及肝脏阶段都是杀寄生虫的[1][2]。

Ganaplacide名称

[ CAS 号 ]:
1261113-96-5

[ 英文名 ]:
Ganaplacide

[英文别名 ]:

85VMN9JU7A
KAF156
MFCD28502124

Ganaplacide生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

[体外研究]

Ganaplacide(KAF156)对恶性疟原虫药物敏感和耐药菌株具有杀血裂殖活性,50%抑制浓度为 6.至 17.4 nM[1]

[体内研究]

Ganaplacide(KAF156)(1-15 mg/kg；口服)在疟疾因果预防小鼠模型中具有完全保护作用[1]对成熟的恶性疟原虫配子细胞表现出杀灭活性,从而阻止寄生虫传播给按蚊[1] 动物模型：小鼠(因果预防性啮齿类动物疟疾模型)[1]剂量：1-15 mg/kg给药：口服。结果：感染前2小时单次口服10 mg KAF156/kg具有完全保护作用。

[参考文献]

[1]. Leong FJ, et al. A first-in-humanrandomized, double-blind, placebo-controlled, single- and multiple-ascendingoral dose study of novel Imidazolopiperazine KAF156 to assess its safety,tolerability, and pharmacokinetics in healthy adult volunteers. AntimicrobAgents Chemother. 2014;58(11):6437-6443.

[2]. Kuhen KL, et al. KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission. Antimicrob Agents Chemother. 2014;58(9):5060-5067.

[3]. Leong FJ, et al. A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel Imidazolopiperazine KAF156 to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers. Antimicrob Agents Chemother. 2014;58(11):6437-6443.

Ganaplacide物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
635.0±55.0 °C at 760 mmHg

[ 分子式 ]:
C₂₂H₂₃F₂N₅O

[ 分子量 ]:
411.45

[ 闪点 ]:
337.8±31.5 °C

[ 精确质量 ]:
411.187073

[ LogP ]:
4.20

[ 蒸汽压 ]:
0.0±1.9 mmHg at 25°C

[ 折射率 ]:
1.639

Ganaplacide

Ganaplacide用途

Ganaplacide名称

Ganaplacide生物活性

Ganaplacide物理化学性质

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