PfPK6-IN-1
PfPK6-IN-1 is a potent and selective PfPK6 inhibitor with an IC50 of 0.3 μM. PfPK6-IN-1 inhibits hemozoin formation, a Plasmodium-specific pathway with IC50 of 13 μM against β-hematin (βH). PfPK6-IN-1 exhibits rapid and broad-spectrum anti-malarial properties, being effective against both chloroquine-sensitive and resistant strains.PfPK6-IN-1 can be used for the study of antimalarial.
For research use only. We do not sell to patients.
- CAS No.: 2417648-94-1
- Formula: C34H41F3N8O2
- Molecular Weight:650.74
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Parasite Isoforms
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Biological Activity
PfPK6-IN-1 (Compound 12) exhibits EC50s of 116 nM against Dd2 asexual blood stage parasites and 210 nM against the P. falciparum 3D7 strain[1].
PfPK6-IN-1 (48 h) is a fast-acting compound active throughout the asexual blood cycle and clears 99.9% of
the parasites (99.9% PCT) within 32.5 h[1].
PfPK6-IN-1 activity is unchanged after PfPK6 knockdown (EC50 of 129 nM in the physiological PK6 levels versus 153 nM in the knockdown) in the Dd2PK6 cKD line[1].
PfPK6-IN-1 (20-850 nM, 13 months) resists the drug resistance of chloroquine resistant P. falciparum Dd2-B2 strain by targeting the digestive vesicle transport proteins (PfCRT and PfMDR1) of the malaria parasite [1].
PfPK6-IN-1 (0-500 nM, 72 h) interaction with chloroquine is antagonistic in 3D7 but synergistic in Dd2[1].
PfPK6-IN-1 (0-32 h) inhibits hemozoin formation by directly inhibiting the formation of β-hematin in P. falciparum 3D7, and increasing the accumulation of toxic hemoglobin in 3D7 parasites[1].
PfPK6-IN-1 (0-72 h) is active against Cambodian and Ugandan P. falciparum isolates[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:The infection of P. bergheiLuc parasites model established in 6 weeks females Swiss webster mice[1]
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Dosage:15 and 50 mg/kg
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Administration:Intravenous injection (i.v.), single dose, 6 hours before infection in prevent group
Intraperitoneal injection (i.p.), once daily, after infection 1-4 days in therapy group -
Result:Prevented the establishment of the infection of P. bergheiLuc parasites in prevent group.
Two mice developed parasitemia and died of malaria between days 12 and 18, while the remaining mice were able to control the disease in therapy group.
Chemical Information
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CAS No. 2417648-94-1
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Molecular Weight 650.74
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Formula C34H41F3N8O2
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SMILES
CN1CCC(C(NC2=CC(OC3=CC=C4C(N(C)C(NC5=CC=C(CN6CCN(CC)CC6)C(C(F)(F)F)=C5)=N4)=C3)=CC=N2)=O)CC1
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)