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1038620-68-6

中文名称 4-[[2-[(反式-4-氨基环己基)氨基]-9-(3-氟苯基)-9H-嘌呤-6-基]氨基]苯基]-1-哌啶基甲酮
英文名称 Purfalcamine
CAS 1038620-68-6
分子式 C29H33FN8O
分子量 528.62
MOL 文件 1038620-68-6.mol
1038620-68-6 结构式 1038620-68-6 结构式

基本信息

中文别名
4-[[2-[(反式-4-氨基环己基)氨基]-9-(3-氟苯基)-9H-嘌呤-6-基]氨基]苯基]-1-哌啶基甲酮
英文别名
Purfalcamine

物理化学性质

沸点784.8±70.0 °C(Predicted)
密度1.42±0.1 g/cm3(Predicted)
储存条件-20°C储存
酸度系数(pKa)10.41±0.70(Predicted)
形态Solid
颜色White to off-white
4-[[2-[(反式-4-氨基环己基)氨基]-9-(3-氟苯基)-9H-嘌呤-6-基]氨基]苯基]-1-哌啶基甲酮价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/05/22HY-1170154-[[2-[(反式-4-氨基环己基)氨基]-9-(3-氟苯基)-9H-嘌呤-6-基]氨基]苯基]-1-哌啶基甲酮
Purfalcamine
1038620-68-61 mg1800元
2025/05/22HY-1170154-[[2-[(反式-4-氨基环己基)氨基]-9-(3-氟苯基)-9H-嘌呤-6-基]氨基]苯基]-1-哌啶基甲酮
Purfalcamine
1038620-68-65mg4500元
2025/05/22HY-1170154-[[2-[(反式-4-氨基环己基)氨基]-9-(3-氟苯基)-9H-嘌呤-6-基]氨基]苯基]-1-哌啶基甲酮
Purfalcamine
1038620-68-610mM * 1mLin DMSO5233元

常见问题列表

生物活性
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。
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 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).

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 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.
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