货号	规格	价格	上海	北京	珠海	重庆	武汉
V45396-1mg	≥98%	￥1790.00 V45396-1mg ￥1790.00 3-5天	0 货期：3-5天	-	-	-	-
V45396-5mg	≥98%	￥4490.00 V45396-5mg ￥4490.00 3-5天	0 货期：3-5天	-	-	-	-
V45396-10mg	≥98%	￥7180.00 V45396-10mg ￥7180.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

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.

靶点：

Plasmodium;Toxoplasma

体内研究：

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).

参考文献：

1. Nobutaka Kato, et al. Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. Nat Chem Biol. 2008 Jun;4(6):347-56.
2. Rajshekhar Y Gaji, et al. Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs. Antimicrob Agents Chemother. 2014 May;58(5):2598-607.

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.892 ml	9.459 ml	18.917 ml
5 mM	0.378 ml	1.892 ml	3.783 ml
10 mM	0.189 ml	0.946 ml	1.892 ml
50 mM	0.038 ml	0.189 ml	0.378 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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