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) shows blood schizonticidal activity with 50% inhibitory concentrations of 6 to 17.4 nM against P. falciparum drug-sensitive and drug-resistant strains^[1].

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

Ganaplacide (KAF156) displays cidal activity against mature Plasmodium falciparum gametocytes and thus blocks parasite transmission to Anopheles mosquitoes^[1].
Ganaplacide (KAF156) (1-15 mg/kg; p.o.) is fully protective in a causal prophylactic mouse model of malaria^[1].

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

411.45

C₂₂H₂₃F₂N₅O

1261113-96-5

FC(C=C1)=CC=C1C2=C(N3C(C(C)(N(C(CN)=O)CC3)C)=N2)NC4=CC=C(F)C=C4

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]