Ganaplacide phosphate  (Synonyms: KAF156 phosphate; GNF156 phosphate)

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

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

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

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

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

607.44

C₂₂H₂₉F₂N₅O₉P₂

3051901-82-4

O=C(CN)N1CCN2C(C1(C)C)=NC(C3=CC=C(C=C3)F)=C2NC4=CC=C(C=C4)F.O=P(O)(O)O.O=P(O)(O)O

Room temperature in continental US; may vary elsewhere.

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

• [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.  [Content Brief]

  [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.  [Content Brief]