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Purfalcamine

CAS No. : 1038620-68-6

MCE 站：Purfalcamine

产品活性：Purfalcamine 是一种具有口服活性，选择性的恶性疟原虫钙依赖性蛋白激酶 1 (PfCDPK1) 抑制剂，IC₅₀ 为 17 nM，EC₅₀ 为 230 nM。Purfalcamine 具有抗疟疾活性，可以引起疟原虫在裂殖体阶段的发育停滞。

研究领域：Anti-infection

作用靶点：Parasite

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 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).

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.

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