Pentamidine dihydrochloride

Research use only, not for human use.

Pentamidine 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 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 at its therapeutic doses inhibited recombinant PRL phosphatases in vitro and inactivated ectopically expressed PRLs in NIH3T3 transfectants with an effective duration more than 24 h after a pulse cell treatment.(In Vivo):Pentamidine at a tolerable dose markedly inhibited the growth of WM9 human melanoma tumors in nude mice coincident with the induction of tumor cell necrosis and is capable of inactivating ectopically expressed PRL-2 in the cancer cells.

Pentamidine (0-10 μg/mL; 6 days; WM9, DU145, C4-2, Hey, WM480, and A549 cells) treatment inhibits the growth of cancer cells in a concentration-dependent manner.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. Cell Viability Assay 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.

Pentamidine (0.25 mg/mouse; intramuscular injection; every 2 days; for 4 weeks; athymic nude mice) treatment markedly inhibits the growth of WM9 human melanoma tumors in nude mice. Animal Model:Athymic nude mice (6 weeks old) injected with WM9 cells 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.

MP-601205 dihydrochloride

Metabolic Enzyme/Protease

Phosphatase

aryl hydrocarbon receptor|GSK-3|CDK1/CyclinB|CDK5/p25

——

——

50357-45-4

413.34

C19H26Cl2N4O2

>98% (HPLC)

——

[Cl-].[Cl-].NC(=[NH2+])c1ccc(OCCCCCOc2ccc(cc2)C(N)=[NH2+])cc1

——

(-20℃)

With Ice Pack

≥ 2 years