Ganaplacide hydrochloride (Synonyms: KAF156 hydrochloride; GNF156 hydrochloride)
目录号: PL08810 纯度: ≥97%
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PL08810-5mg 5mg ¥9322.00 请登录
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中文名称
Ganaplacide hydrochloride
英文名称
Ganaplacide hydrochloride
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)
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。
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.
性状
Solid
IC50 & Target[1][2]
Plasmodium
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.
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.
运输条件
Room temperature in continental US; may vary elsewhere.
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)
ClinicalTrial
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.
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
搜索质检报告(COA)

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。

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