| Description | Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an aromatic diamidine agent with activity against a number of microorganisms including protozoa (Trypanosoma brucei, Leishmania spp., and Babesia spp.) and fungi (Pneumocystis jirovecii). Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases and phosphatase of regenerating liver inhibitor. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. |
| In vitro | Pentamidine 在其治疗剂量下，能抑制体外重组PRL磷酸酶，并在NIH3T3转染细胞中使异位表达的PRL失活，有效作用时间在脉冲细胞处理后超过24小时[3]。 |
| In vivo | Pentamidine 以可耐受剂量显著抑制裸鼠体内WM9人类黑色素瘤肿瘤的生长，同时伴随着肿瘤细胞坏死的诱导，并能够在癌细胞中失活异位表达的PRL-2[3]。 |
| Target activity | Leishmania infantum:2.5 μM |
| Synonyms | 喷他脒二盐酸盐, MP-601205 dihydrochloride |
| molecular weight | 413.34 |
| Molecular formula | C19H26Cl2N4O2 |
| CAS | 50357-45-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 4.13 mg/mL (10 mM), Sonication is recommended. |
| References | 1. Nguewa, P.A., et al., Pentamidine is an antiparasitic and apoptotic drug that selectively modifies ubiquitin. Chem Biodivers, 2005. 2(10): p. 1387-400. 2. 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. 3. Pathak MK, et al. Pentamidine is an inhibitor of PRL phosphatases with anticancer activity. Mol Cancer Ther. 2002 Dec;1(14):1255-64. 4. Sands M, et al. Pentamidine: a review. Rev Infect Dis. 1985 Sep-Oct;7(5):625-34. |