4,4'-[1,5-pentanediylbis(oxy)]bisbenzenecarboxamidine dimethylsulphonate
Names
[ CAS No. ]:
6823-79-6
[ Name ]:
4,4'-[1,5-pentanediylbis(oxy)]bisbenzenecarboxamidine dimethylsulphonate
[Synonym ]:
4,4'-pentanediyldioxy-bis-benzamidine,bis-methanesulfonate
4,4'-Pentandiyldioxy-bis-benzamidin,Bis-methansulfonat
pentamidine dimethansulfonate
Biological Activity
[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].
[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]
Chemical & Physical Properties
[ Molecular Formula ]:
C20H28N4O5S
[ Molecular Weight ]:
436.52500
[ Exact Mass ]:
436.17800
[ PSA ]:
180.95000
[ LogP ]:
5.06770
Safety Information