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

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

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
中文同义词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
英文同义词Purfalcamine;Methanone, [4-[[2-[(trans-4-aminocyclohexyl)amino]-9-(3-fluorophenyl)-9H-purin-6-yl]amino]phenyl]-1-piperidinyl-
CAS号1038620-68-6
分子式C29H33FN8O
分子量528.62
EINECS号
相关类别
Mol文件1038620-68-6.mol
结构式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 结构式

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 性质

沸点784.8±70.0 °C(Predicted)
密度1.42±0.1 g/cm3(Predicted)
储存条件Store at -20°C
形态固体
酸度系数(pKa)10.41±0.70(Predicted)
颜色白色至米白色

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 用途与合成方法

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。

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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2026/09/15HY-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
2026/09/15HY-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

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 上下游产品信息

"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"相关产品信息
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