1. Anti-infection
  2. Parasite
  3. PfPK6-IN-1

PfPK6-IN-1 是一种强效且选择性的 PfPK6 抑制剂,其 IC50 值为 0.3 μM。PfPK6-IN-1 能抑制疟原虫色素形成,一种疟原虫特异性的特有的血红素解毒途径,对β-血红素 (βH) 的 IC50 值为 13 μM。PfPK6-IN-1 具有快速且广谱的抗疟疾特性,对敏感型和耐药型疟原虫菌株均有效。PfPK6-IN-1 可用于抗疟疾剂的研究。

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PfPK6-IN-1

PfPK6-IN-1 Chemical Structure

CAS No. : 2417648-94-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PfPK6-IN-1 is a potent and selective PfPK6 inhibitor with an IC50 of 0.3 μM. PfPK6-IN-1 inhibits hemozoin formation, a Plasmodium-specific pathway with IC50 of 13 μM against β-hematin (βH). PfPK6-IN-1 exhibits rapid and broad-spectrum anti-malarial properties, being effective against both chloroquine-sensitive and resistant strains.PfPK6-IN-1 can be used for the study of antimalarial[1].

体外研究
(In Vitro)

PfPK6-IN-1 (Compound 12) 对 Dd2 无性血液期寄生虫的 EC50 为 116 nM,对恶性疟原虫(P. falciparum) 3D7 株的 EC50 为 210 nM[1]
PfPK6-IN-1 (48 h) 是一种速效化合物,在整个无性血液周期中均有活性,能在 32.5 小时内清除 99.9%的寄生虫[1]
PfPK6-IN-1 在 Dd2PK6 cKD 株中,PfPK6 敲低后,PfPK6-IN-1 的活性未发生改变 (生理 PK6水平下的 EC50 为 129 nM,敲低情况下为 153 nM)[1]
PfPK6-IN-1 (20-850 nM, 13 months) 通过靶向疟原虫消化泡转运蛋白 (PfCRT和PfMDR1),从而抵抗 Dd2 株的耐药性[1]
PfPK6-IN-1 (0-500 nM, 72 h) 与氯喹的相互作用在 3D7 株中呈拮抗关系,在 Dd2 株中呈协同关系[1]
PfPK6-IN-1 (0-32 h) 通过直接抑制恶性疟原虫 P. falciparum D7 中 β-hematin 的形成,并增加 3D7 寄生虫中毒性血红蛋白的积累,从而抑制疟色素的形成[1]
PfPK6-IN-1 (0-72 h) 对柬埔寨和乌干达的恶性疟原虫 P. falciparum 分离株具有活性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

PfPK6-IN-1 (Compound 12) (15-50 mg/kg, i.v. 或 i.p.,单次给药或每日一次连续 4 天给药) 能完全预防小鼠对 < i>P. berghei 的感染,部分抑制小鼠体内已有的 < i>P. berghei 的感染[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: The infection of P. berghei Luc parasites model established in 6 weeks females Swiss webster mice[1]
Dosage: 15 and 50 mg/kg
Administration: Intravenous injection (i.v.), single dose, 6 hours before infection in prevent group
Intraperitoneal injection (i.p.), once daily, after infection 1-4 days in therapy group
Result: Prevented the establishment of the infection of P. berghei Luc parasites in prevent group.
Two mice developed parasitemia and died of malaria between days 12 and 18, while the remaining mice were able to control the disease in therapy group.
分子量

650.74

Formula

C34H41F3N8O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

PfPK6-IN-1 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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