Ganaplacide
Ganaplacide (KAF156) is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite.
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- No. CAS: 1261113-96-5
- Fòrmula: C22H23F2N5O
- Peso molecular:411.45
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | CC50 |
>12 μM
Compound: 22
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Cytotoxicity against mouse BA/F3 cells
Cytotoxicity against mouse BA/F3 cells
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[PMID: 22524250] |
| CHO | CC50 |
>12 μM
Compound: 22
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Cytotoxicity against CHO cells
Cytotoxicity against CHO cells
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[PMID: 22524250] |
| CHO | IC50 |
13.4 μM
Compound: 22
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Inhibition of human ERG channel expressed in CHO cells by patch clamp assay
Inhibition of human ERG channel expressed in CHO cells by patch clamp assay
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[PMID: 22524250] |
| HEK-293T | CC50 |
>12 μM
Compound: 22
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Cytotoxicity against human 293T cells
Cytotoxicity against human 293T cells
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[PMID: 22524250] |
| HeLa | CC50 |
>12 μM
Compound: 22
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Cytotoxicity against human HeLa cells
Cytotoxicity against human HeLa cells
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[PMID: 22524250] |
| HEp-2 | CC50 |
>12 μM
Compound: 22
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Cytotoxicity against human Hep2 cells
Cytotoxicity against human Hep2 cells
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[PMID: 22524250] |
| Huh-7 | CC50 |
>12 μM
Compound: 22
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Cytotoxicity against human HuH7 cells
Cytotoxicity against human HuH7 cells
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[PMID: 22524250] |
Ganaplacide (KAF156) shows blood schizonticidal activity with 50% inhibitory concentrations of 6 to 17.4 nM against P. falciparum drug-sensitive and drug-resistant strains[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ganaplacide (KAF156) (1-15 mg/kg; p.o.) is fully protective in a causal prophylactic mouse model of malaria[1].
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:A single oral dose of 10 mg of KAF156/kg administered 2 h before infection was fully protective.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1261113-96-5
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Peso molecular 411.45
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Fòrmula C22H23F2N5O
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SMILES
FC(C=C1)=CC=C1C2=C(N3C(C(C)(N(C(CN)=O)CC3)C)=N2)NC4=CC=C(F)C=C4
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Synonyms
KAF156; GNF156
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. 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]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ganaplacide Related Classifications
HY-108024 Related Classifications
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