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Pentamidine dihydrochloride (Synonyms: 喷他脒二盐酸盐; MP-601205 dihydrochloride)
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。
Pentamidine dihydrochloride Chemical Structure
CAS No. : 50357-45-4
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
Pentamidine dihydrochloride 的其他形式现货产品:
Pentamidine isethionate
| 生物活性 |
Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4].
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IC50 & Target |
IC50: 2.5 μM (Leishmania infantum)[2]
Protein tyrosine phosphatases (PTPases)[1]
Phosphatase of regenerating liver (PRL)[1]
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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 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[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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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| Clinical Trial |
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| 分子量 |
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| Formula |
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| CAS 号 |
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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
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Pathak MK, et al. Pentamidine is an inhibitor of PRL phosphatases with anticancer activity. Mol Cancer Ther. 2002 Dec;1(14):1255-64.
[2]. Nguewa, P.A., et al., Pentamidine is an antiparasitic and apoptotic drug that selectively modifies ubiquitin. Chem Biodivers, 2005. 2(10): p. 1387-400.
[3]. Sands M, et al. Pentamidine: a review. Rev Infect Dis. 1985 Sep-Oct;7(5):625-34.
[4]. David C. Bean, et al. Pentamidine: a drug to consider re-purposing in the targeted treatment of multi-drug resistant bacterial infections? J Lab Precis Med 2017;2:49.
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