Pentamidine

SKU: orb1219669

Description

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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 100-33-4
• MW: 340.42
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₄N₄O₂
• SMILES: NC(=N)c1ccc(OCCCCCOc2ccc(cc2)C(N)=N)cc1
• Target: Antifungal

Bioactivity

• 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. Animal model: Athymic nude mice (6 weeks old) injected with WM9 cells. 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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• 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. 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 Assay 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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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Antifungal