产品
编 号：F016661
分子式：C29H33FN8O
分子量：528.62
分子式：C29H33FN8O
分子量：528.62
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规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 1038620-68-6
产品详情
生物活性：
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.
体内研究：
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 Cmax 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 (Cmax) of 2.6 μM with a half-life of 3.1 hours.
体外研究：
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 EC50s of 171-259 nM for P. falciparum strains (3D7, Dd2, FCB, HB3 and W2), which indicates effectiveness against drug-resistant parasites. 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).
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.
体内研究：
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 Cmax 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 (Cmax) of 2.6 μM with a half-life of 3.1 hours.
体外研究：
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 EC50s of 171-259 nM for P. falciparum strains (3D7, Dd2, FCB, HB3 and W2), which indicates effectiveness against drug-resistant parasites. 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).
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