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. Nr.: 3051901-82-4
- Formel: C22H29F2N5O9P2
- Molecular Weight:607.44
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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.
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. Nr. 3051901-82-4
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Molecular Weight 607.44
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Ganaplacide phosphate Related Classifications
HY-108024B Related Classifications
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