6823-79-6
6823-79-6 structure
- Name: 4,4'-[1,5-pentanediylbis(oxy)]bisbenzenecarboxamidine dimethylsulphonate
- Chemical Name: pentamidine dimethanesulfonate
- CAS Number: 6823-79-6
- Molecular Formula: C20H28N4O5S
- Molecular Weight: 436.52500
- Catalog: Signaling Pathways Anti-infection Bacterial
- Create Date: 2017-07-11 21:01:58
- Modify Date: 2024-04-12 16:16:48
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Pentamidine (MP-601205) dimesylate is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dimesylate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dimesylate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dimesylate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4].
| Name | pentamidine dimethanesulfonate |
|---|---|
| Synonyms |
4,4'-pentanediyldioxy-bis-benzamidine,bis-methanesulfonate
4,4'-Pentandiyldioxy-bis-benzamidin,Bis-methansulfonat pentamidine dimethansulfonate |
| Description | Pentamidine (MP-601205) dimesylate is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dimesylate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dimesylate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dimesylate 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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| Related Catalog | |
| In Vitro | Pentamidine (0-10 µg/mL; 6 days; WM9, DU145, C4-2, Hey, WM480, and A549 cells) dimesylate 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]. 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. |
| In Vivo | Pentamidine (0.25 mg/mouse; intramuscular injection; every 2 days; for 4 weeks; athymic nude mice) dimesylate 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. |
| References |
[3]. Sands M, et al. Pentamidine: a review. Rev Infect Dis. 1985 Sep-Oct;7(5):625-34. |
| Molecular Formula | C20H28N4O5S |
|---|---|
| Molecular Weight | 436.52500 |
| Exact Mass | 436.17800 |
| PSA | 180.95000 |
| LogP | 5.06770 |
| RIDADR | UN 3249 |
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