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Art. -Nr.: HY-108024

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Ganaplacide

(Synonyms: KAF156; GNF156)

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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CAS. Nr.: 1261113-96-5
Formel: C₂₂H₂₃F₂N₅O
Molecular Weight:411.45

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

Ganaplacide Chemical Structure

CAS. Nr.: 1261113-96-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Parasite Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	CC₅₀	>12 μM Compound: 22	Cytotoxicity against mouse BA/F3 cells Cytotoxicity against mouse BA/F3 cells	[PMID: 22524250]
CHO	CC₅₀	>12 μM Compound: 22	Cytotoxicity against CHO cells Cytotoxicity against CHO cells	[PMID: 22524250]
CHO	IC₅₀	13.4 μM Compound: 22	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	[PMID: 22524250]
HEK-293T	CC₅₀	>12 μM Compound: 22	Cytotoxicity against human 293T cells Cytotoxicity against human 293T cells	[PMID: 22524250]
HeLa	CC₅₀	>12 μM Compound: 22	Cytotoxicity against human HeLa cells Cytotoxicity against human HeLa cells	[PMID: 22524250]
HEp-2	CC₅₀	>12 μM Compound: 22	Cytotoxicity against human Hep2 cells Cytotoxicity against human Hep2 cells	[PMID: 22524250]
Huh-7	CC₅₀	>12 μM Compound: 22	Cytotoxicity against human HuH7 cells Cytotoxicity against human HuH7 cells	[PMID: 22524250]

In Vitro

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.

In Vivo

Ganaplacide (KAF156) displays cidal activity against mature Plasmodium falciparum gametocytes and thus blocks parasite transmission to Anopheles mosquitoes^[1].
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.

Animal Model:

Mice (causal prophylactic rodent malaria model)^[1]
Dosage:

1-15 mg/kg
Administration:

p.o.
Result:

A single oral dose of 10 mg of KAF156/kg administered 2 h before infection was fully protective.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1261113-96-5
Molecular Weight 411.45
Formel C₂₂H₂₃F₂N₅O
SMILES

FC(C=C1)=CC=C1C2=C(N3C(C(C)(N(C(CN)=O)CC3)C)=N2)NC4=CC=C(F)C=C4
Synonyms

KAF156; GNF156
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Reinheit & Dokumentation
Verweise

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Ganaplacide

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Ganaplacide Related Classifications

HY-108024 Related Classifications