4,4'-[1,5-pentanediylbis(oxy)]bisbenzenecarboxamidine dimethylsulphonate
4,4'-[1,5-pentanediylbis(oxy)]bisbenzenecarboxamidine dimethylsulphonate Basic information
- Product Name:
- 4,4'-[1,5-pentanediylbis(oxy)]bisbenzenecarboxamidine dimethylsulphonate
- Synonyms:
-
- 4,4'-[1,5-pentanediylbis(oxy)]bisbenzenecarboxamidine dimethylsulphonate
- PENTAMIDINE DIMETHANESULFONATE
- pentamidine mesylate
- Lomidine
- Pentamidine dimesylate
- CAS:
- 6823-79-6
- MF:
- C21H32N4O8S2
- MW:
- 532.63078
- EINECS:
- 229-898-4
- Mol File:
- 6823-79-6.mol
4,4'-[1,5-pentanediylbis(oxy)]bisbenzenecarboxamidine dimethylsulphonate Usage And Synthesis
Uses
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].
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. |
IC 50
Trypanosoma; Leishmania
References
[1] Pathak MK, et al. Pentamidine is an inhibitor of PRL phosphatases with anticancer activity. Mol Cancer Ther. 2002 Dec;1(14):1255-64. PMID:12516958
[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. DOI:10.1002/cbdv.200590111
[3] Sands M, et al. Pentamidine: a review. Rev Infect Dis. 1985 Sep-Oct;7(5):625-34. DOI:10.1093/clinids/7.5.625
[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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