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.
For research use only. We do not sell to patients.
- CAS No.: 1261113-96-5
- Formula: C22H23F2N5O
- Molecular Weight:411.45
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Parasite Isoforms
More
Biological Activity
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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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1261113-96-5
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Molecular Weight 411.45
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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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