Bioactivity | Ganaplacide (KAF156) is a first-in-class,orally active imidazolopiperazine antimalarial agent.Ganaplacide is active against a broad range of Plasmodiumspecies, including drug-resistant parasites. Ganaplacide is parasiticidalagainst both asexual and sexual blood stages as well as the liver stages of theparasite[1][2]. |
Invitro | 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]。 |
In Vivo | 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]。 Animal Model: |
Name | Ganaplacide |
CAS | 1261113-96-5 |
Formula | C22H23F2N5O |
Molar Mass | 411.45 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Leong FJ, et al. A first-in-humanrandomized, double-blind, placebo-controlled, single- and multiple-ascendingoral dose study of novel Imidazolopiperazine KAF156 to assess its safety,tolerability, and pharmacokinetics in healthy adult volunteers. AntimicrobAgents Chemother. 2014;58(11):6437-6443. [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. [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. |