| Identification | Back Directory | [Name]
Ethanone, 2-amino-1-[2-(4-fluorophenyl)-3-[(4-fluorophenyl)amino]-5,6-dihydro-8,8-dimethylimidazo[1,2-a]pyrazin-7(8H)-yl]-, hydrochloride (1:1) | [CAS]
2751586-94-2 | [Synonyms]
KAF156/GNF156
2-Amino-1-(2-(4-fluorophenyl)-3-((4-fluorophenyl)amino)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)ethan-1-one hydrochloride | [Molecular Formula]
C22H23F2N5O.ClH | [MOL File]
2751586-94-2.mol | [Molecular Weight]
447.91 |
| Hazard Information | Back Directory | [Uses]
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[1][2]. | [in vivo]
KAF156 displays cidal activity against mature Plasmodium falciparum gametocytes and thus blocks parasite transmission to Anopheles mosquitoes[1].
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Ganaplacide (KAF156) hydrochloride (1-15 mg/kg; p.o.) is fully protective in a causal prophylactic mouse model of malaria[1]. | Animal Model: | Mice (causal prophylactic rodent malaria model)[1] | | Dosage: | 1-15 mg/kg | | Administration: | p.o. | | Result: | A single oral dose of 10 mg of KAF156/kg administered 2 h before infection was fully protective.
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| [IC 50]
Plasmodium | [References]
[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. DOI:10.1128/AAC.02727-13
[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. DOI:10.1128/AAC.03478-14 |
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