ChemicalBook CAS DataBase List 1038620-68-6

1038620-68-6

Name	Purfalcamine
CAS	1038620-68-6
Molecular Formula	C29H33FN8O
MDL Number	MFCD32857138
Molecular Weight	528.62
MOL File	1038620-68-6.mol

Chemical Properties

Boiling point	784.8±70.0 °C(Predicted)
density	1.42±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
form	Solid
pka	10.41±0.70(Predicted)
color	White to off-white

Hazard Information

Biological Activity

Purfalcamine is an orally active and selective inhibitor of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) with IC50 of 17 nM and EC50 of 230 nM. It has antimalarial activity and can cause developmental arrest in the schizont stage of Plasmodium.

in vitro

Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3).
Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, parasite level remains stable and then begins dropping.
Purfalcamine inhibits proliferation with EC ₅₀ s of 171-259 nM for P. falciparum strains (3D7, Dd2, FCB, HB3 and W2), which indicate effectiveness against drug-resistant parasites.
Given that the EC ₅₀ value for P. falciparum (3D7) is 230 nM, Purfalcamine shows a therapeutic window ranging from 23-fold to 36-fold (EC ₅₀ s for CHO=12.33 μM, HEp2=7.235 μM, HeLa=7.029 μM and Huh7 =5.476 μM).

in vivo

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

Animal Model:	Male BALB/c mice, 7 weeks of age with the malaria parasite
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-ol d male Balb/c mice (22-25 g)
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	Orally gavage
Result:	Exhibited a maximum plasma exposure (C _max ) of 2.6 μM with a half-life of 3.1 hours.

storage

Store at -20°C

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