Ganaplacide  (Synonyms: KAF156; GNF156)

Ganaplacide (KAF156) is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite^[1][2].

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]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Ganaplacide (KAF156) (1-15 mg/kg; p.o.) is fully protective in a causal prophylactic mouse model of malaria^[1]. Ganaplacide (KAF156) 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]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

411.45

C₂₂H₂₃F₂N₅O

1261113-96-5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. 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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]