1038620-68-6
1038620-68-6 結構式
物理化學性質
常見問題列表
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 indicates 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).
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-old 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. |