Identification | Back Directory | [Name]
4,4'-[1,5-pentanediylbis(oxy)]bisbenzenecarboxamidine dimethylsulphonate | [CAS]
6823-79-6 | [Synonyms]
Lomidine pentamidine mesylate Pentamidine dimesylate PENTAMIDINE DIMETHANESULFONATE 4,4'-[1,5-pentanediylbis(oxy)]bisbenzenecarboxamidine dimethylsulphonate | [EINECS(EC#)]
229-898-4 | [Molecular Formula]
C21H32N4O8S2 | [MDL Number]
MFCD01667908 | [MOL File]
6823-79-6.mol | [Molecular Weight]
532.631 |
Hazard Information | Back Directory | [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. |
|
|