Pentamidine dihydrochloride(Synonyms: 喷他脒二盐酸盐; MP-601205 dihydrochloride)

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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(Synonyms: 喷他脒二盐酸盐; MP-601205 dihydrochloride)

Pentamidine dihydrochloride Chemical Structure

CAS No. : 50357-45-4

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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].

IC50 & Target

IC50: 2.5 μM (Leishmania infantum)[2]
Protein tyrosine phosphatases (PTPases)[1]
Phosphatase of regenerating liver (PRL)[1]
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.

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.

Clinical Trial

分子量

413.34

Formula

C19H26Cl2N4O2
CAS 号

50357-45-4
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.
参考文献

  • [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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