Pentamidine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

喷他脒是一种抗真菌和抗原虫剂，通过与双链 DNA 富含 AT 的区域和 DNA 小沟结合，直接与病原体基因组相互作用，从而干扰 DNA 复制。喷脒脒可有效治疗冈比亚锥虫病的血淋巴阶段，耐锑利什曼病和卡氏肺孢子虫肺炎。

Pentamidine is an antifungal and antiprotozoal agent, interacting directly with the pathogen genome by binding to AT-rich regions of duplex DNA and the minor groove of DNA, thereby interfering with DNA replication.Pentamidine is effective in therapy for the hemolymphatic stage of Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia.

Pentamidine (0-10 μg/mL; 6 days; WM9, DU145, C4-2, Hey, WM480, and A549 cells) treatment inhibits the growth of cancer cells in a concentration-dependent manner.The cytotoxic properties of Pentamidine isethionate towards the promastigotes of the protozoan parasite Leishmania infantum is determined. The leishmanicidal activity of Pentamidine isethionate is 60 times higher after 72 h of incubation than that of Cisplatin. Pentamidine isethionate induces a higher amount of programmed cell death (PCD) than Cisplatin, which is associated with inhibition of DNA synthesis and cell-cycle arrest in the G2/M phase. Binding of Pentamidine isethionate to calf-thymus DNA (CT-DNA) induces conformational changes in the DNA double helix, consistent with a B-->A transition. The interaction of Pentamidine isethionate with ubiquitin leads to a 6% increase in the beta-sheet content of the protein. Cell Viability AssayCell Line:WM9, DU145, C4-2, Hey, WM480, and A549 cells Concentration:0-10 μg/mL Incubation Time:6 days Result:The growth of all six of the cell lines in culture was inhibited in a concentration-dependent manner with complete growth inhibition of the cell lines occurring at 10 μg/mL.

Pentamidine (0.25 mg/mouse; intramuscular injection; every 2 days; for 4 weeks; athymic nude mice) treatment markedly inhibits the growth of WM9 human melanoma tumors in nude mice. Animal Model:Athymic nude mice (6 weeks old) injected with WM9 cellsDosage:0.25 mg/mouse Administration:Intramuscular injection; every 2 days; for 4 weeks Result:Markedly inhibited the growth of WM9 human melanoma tumors in nude mice.

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Microbiology/Virology

Antifungal

antifungal

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100-33-4

340.42

C19H24N4O2

>98% (HPLC)

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NC(=N)c1ccc(OCCCCCOc2ccc(cc2)C(N)=N)cc1

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(-20℃)

With Ice Pack

≥ 2 years