| Hazard Information | Back Directory | [Description]
KAR425 is a bipyrrole tambjamines with antimalarial activity against multidrug-resistant P. yoelii in mice. | [Uses]
KAR425 is a potent and orally active antimalarial agent. KAR425 shows antimalarial activity against the Chloroquine-sensitive (CQS) D6, the Chloroquine-resistant (CQR) Dd2, and 7G8 strains of Plasmodium falciparum, with IC50 values of 62 nM, 55 nM, and 60 nM, respectively[1]. | [in vivo]
KAR425 (25-50 mg/kg/day; Oral gavage; once daily; for 4 days) provides 100% protection to malaria-infected mice until day 28[1]. | Animal Model: | 4- to 5-week-old female CF1 mice were infected intravenously with P. yoelii[1]. | | Dosage: | 25 and 50 mg/kg/day | | Administration: | Oral gavage; once daily; for four successive days | | Result: | Provided parasite-free cures on day 28 (100% protection to malaria-infected mice) at 25 and 50 mg/kg/day.
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| [References]
[1] Papireddy Kancharla, et al. Synthesis and Structure-Activity Relationships of Tambjamines and B-Ring Functionalized Prodiginines as Potent Antimalarials. J Med Chem. 2015 Sep 24;58(18):7286-309. DOI:10.1021/acs.jmedchem.5b00560 |
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