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Pentamidine isethionate

SKU: orb1226341

Description

Pentamidine isethionate is an antimicrobial agent for prevention and treatment of Pneumocystis pneumonia (PCP) caused by Pneumocystis jirovecii.(In Vitro):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.(In Vivo):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.

Images & Validation

Key Properties

CAS Number140-64-7
MW592.68
Purity>98% (HPLC)
FormulaC23H36N4O10S2
SMILESC1=CC(=CC=C1C(=N)N)OCCCCCOC2=CC=C(C=C2)C(=N)N.C(CS(=O)(=O)O)O.C(CS(=O)(=O)O)O
TargetOthers
SolubilityDMSO: 100mg/ml(168.73 mM);Water: 100mg/ml(168.73 mM);Ethanol: <1mg/ml

Bioactivity

In Vivo
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.
In Vitro
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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Pentamidine Isethionate | Pentamidine isethionate salt | Pentamidine diisethionate

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    140-64-7

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Pentamidine isethionate (orb1226341)

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500 mg
100 mg
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