| 中文名称 |
Ganaplacide hydrochloride
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| 英文名称 |
Ganaplacide hydrochloride
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| 包装储存 |
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| 详情描述 |
Ganaplacide (KAF156) hydrochloride 是一种首创的具有口服活性的咪唑哌嗪类抗疟药 (antimalarial)。Ganaplacide hydrochloride 对多种疟原虫有活性,包括耐药寄生虫。Ganaplacide hydrochloride 对无性和有性血液阶段以及肝脏阶段都有杀虫作用。
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| 产品详情 |
Ganaplacide (KAF156) hydrochloride 是一种首创的具有口服活性的咪唑哌嗪类抗疟药 (antimalarial)。Ganaplacide hydrochloride 对多种疟原虫有活性,包括耐药寄生虫。Ganaplacide hydrochloride 对无性和有性血液阶段以及肝脏阶段都有杀虫作用。
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| 生物活性 |
Ganaplacide (KAF156) hydrochloride is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide hydrochloride is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide hydrochloride is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
Plasmodium
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| 体外研究(In Vitro) |
Ganaplacide (KAF156) hydrochloride shows blood schizonticidal activity with 50% inhibitory concentrations of 6 to 17.4 nM against P. falciparum drug-sensitive and drug-resistant strains. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
KAF156 displays cidal activity against mature Plasmodium falciparum gametocytes and thus blocks parasite transmission to Anopheles mosquitoes.
Ganaplacide (KAF156) hydrochloride (1-15 mg/kg; p.o.) is fully protective in a causal prophylactic mouse model of malaria. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| ClinicalTrial |
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| 参考文献 |
[1]. 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.[2]. 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.
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| 溶解度数据 |
In Vitro: DMSO : 100 mg/mL (223.26 mM; Need ultrasonic)H2O : 33.33 mg/mL (74.41 mM; Need ultrasonic)配制储备液
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[1]. 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.[2]. 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.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。