Pentamidine dihydrochloride (MP-601205 dihydrochloride) 是一种抗微生物剂,会干扰 DNA 的生物合成。Pentamidine dihydrochloride 抑制寄生虫Leishmania infantum,IC50为 2.5 μM。Pentamidine dihydrochloride 是一种有效的选择性蛋白酪氨酸磷酸酶 (PTPases) 和再生肝磷酸酶 (PRL) 抑制剂。Pentamidine dihydrochloride 可用于冈比亚锥虫病,抗锑利什曼病和卡氏肺孢子虫肺炎的研究。抗肿瘤活性,抗菌活性。
生物活性 | Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibitsparasiteLeishmaniainfantumwith anIC50of 2.5 μM. Pentamidine dihydrochloride is a potent and selectiveprotein tyrosine phosphatases(PTPases)andphosphataseof regenerating liver (PRL)inhibitor. Pentamidine dihydrochloride has the potential forGambian trypanosomiasis, antimony-resistantleishmaniasis, andPneumocystis cariniipneumonia treatment. Antitumor and antibacterial activities[1][2][3][4]. |
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体外研究 (In Vitro) | 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[1]. The cytotoxic properties of Pentamidine isethionate towards the promastigotes of the protozoan parasiteLeishmania infantumis 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[2].
Cell Viability Assay[1] Cell 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. |
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体内研究 (In Vivo) | 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[1].
Animal Model: | Athymic nude mice (6 weeks old) injected with WM9 cells[1] | Dosage: | 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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中文名称 | 喷他脒二盐酸盐;喷它咪二盐酸盐;戊烷脒二盐酸盐;戊脘脒二盐酸盐 |
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. |