For research use only. Not for therapeutic Use.
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].
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[1].
KAF156 displays cidal activity against mature Plasmodium falciparum gametocytes and thus blocks parasite transmission to Anopheles mosquitoes[1].?
Ganaplacide (KAF156) hydrochloride (1-15 mg/kg; p.o.) is fully protective in a causal prophylactic mouse model of malaria[1].
| Catalog Number | I045654 |
| CAS Number | 2751586-94-2 |
| Synonyms | 2-amino-1-[3-(4-fluoroanilino)-2-(4-fluorophenyl)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7-yl]ethanone;hydrochloride |
| Molecular Formula | C22H24ClF2N5O |
| Purity | ≥95% |
| InChI | InChI=1S/C22H23F2N5O.ClH/c1-22(2)21-27-19(14-3-5-15(23)6-4-14)20(26-17-9-7-16(24)8-10-17)28(21)11-12-29(22)18(30)13-25;/h3-10,26H,11-13,25H2,1-2H3;1H |
| InChIKey | XCXQBXGWYRFISY-UHFFFAOYSA-N |
| SMILES | CC1(C2=NC(=C(N2CCN1C(=O)CN)NC3=CC=C(C=C3)F)C4=CC=C(C=C4)F)C.Cl |
| Reference | [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. |
