Ganaplacide 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.
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- CAS No.: 3051901-82-4
- Formule: C22H29F2N5O9P2
- Masse moléculaire:607.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
In Vitro
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice (causal prophylactic rodent malaria model)[1]
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Dosage:1-15 mg/kg
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Administration:p.o.
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Result:Was fully protective (a single oral dose of 10 mg of KAF156/kg administered 2 h before infection).
Chemical Information
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CAS No. 3051901-82-4
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Masse moléculaire 607.44
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Formule C22H29F2N5O9P2
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SMILES
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
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Synonyms
KAF156 phosphate; GNF156 phosphate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)