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Purfalcamine 

Cat. No.: HY-117015 Purity: 99.71%
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Purfalcamine is an orally active, selective Plasmodium falciparum, calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage.

For research use only. We do not sell to patients.

Purfalcamine Chemical Structure

Purfalcamine Chemical Structure

CAS No. : 1038620-68-6

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10 mM * 1  mL in DMSO USD 814 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Purfalcamine is an orally active, selective Plasmodium falciparum, calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2].

In Vitro

Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1].
Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, parasite levels remains stable and then began dropping[1].
Purfalcamine inhibits proliferation with EC50s (171-259 nM) for P. falciparum strains (3D7, Dd2, FCB, HB3 and W2), which indicates effectiveness against drug-resistant parasites[1].
Given that the EC50 value for P. falciparum (3D7) is 230 nM, Purfalcamine shows a therapeutic window ranging from 23-fold to 36-fold (EC50s for CHO=12.33 μM, HEp2=7.235 μM, HeLa=7.029 μM and Huh7=5.476 μM)[1].

In Vivo

Purfalcamine (10 mg/kg; oral gavage; BID; for 6 days) demonstrates a delay in the onset of parasitemia in treated mice[1].
Purfalcamine (20 mg/kg; orally gavage) exhibits a Cmax of 2.6 μM with a half-life of 3.1 hours[1].

Animal Model: Male BALB/c mice, 7 weeks of age with the malaria parasite[1]
Dosage: 10 mg/kg
Administration: Oral gavage; BID; for 6 days
Result: Demonstrated a delay in the onset of parasitemia in treated mice when compared with control mice.
Animal Model: Five- to six-week-old male Balb/c mice (22-25 g)[1]
Dosage: 20 mg/kg (Pharmacokinetic Analysis)
Administration: Orally gavage
Result: Exhibited a maximum plasma exposure (Cmax) of 2.6 μM with a half-life of 3.1 hours.
Molecular Weight

528.62

Formula

C₂₉H₃₃FN₈O

CAS No.

1038620-68-6

SMILES

O=C(C1=CC=C(NC2=C3N=CN(C4=CC=CC(F)=C4)C3=NC(N[[email protected]]5CC[[email protected]](N)CC5)=N2)C=C1)N6CCCCC6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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Keywords:

PurfalcamineParasiteorallyPlasmodiumfalciparumcalcium-dependentproteinkinase1PfCDPK1antimalarialmalariaparasitesTgCDPK33D7Dd2FCBHB3W2Inhibitorinhibitorinhibit

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Purfalcamine
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HY-117015
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