1. Anti-infection
    Metabolic Enzyme/Protease
  2. Parasite
    Fungal
    Phosphatase
    Bacterial
    Antibiotic
  3. Pentamidine isethionate

Pentamidine isethionate (Synonyms: MP-601205 isethionate)

Cat. No.: HY-B0537B Purity: 99.82%
Handling Instructions

Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.

For research use only. We do not sell to patients.

Pentamidine isethionate Chemical Structure

Pentamidine isethionate Chemical Structure

CAS No. : 140-64-7

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Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
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10 mM * 1 mL
ready for reconstitution
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Estimated Time of Arrival: December 31
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50 mg USD 60 In-stock
Estimated Time of Arrival: December 31
100 mg USD 96 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Pentamidine isethionate:

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Description

Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4].

IC50 & Target

IC50: 2.5 μM (Leishmania infantum)[2]
Protein tyrosine phosphatases (PTPases)[1]
Phosphatase of regenerating liver (PRL)[1]

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[1].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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.
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

592.68

Formula

C₂₃H₃₆N₄O₁₀S₂

CAS No.
SMILES

N=C(C1=CC=C(OCCCCCOC2=CC=C(C(N)=N)C=C2)C=C1)N.OCCS(=O)(O)=O.OCCS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (168.73 mM; Need ultrasonic)

DMSO : 100 mg/mL (168.73 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6873 mL 8.4363 mL 16.8725 mL
5 mM 0.3375 mL 1.6873 mL 3.3745 mL
10 mM 0.1687 mL 0.8436 mL 1.6873 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.51 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.51 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.51 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.82%

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Keywords:

PentamidineMP-601205MP601205MP 601205ParasiteFungalPhosphataseBacterialAntibioticKidneyDNAbiosyntheticsPneumocystiscariniipneumoniacell-cyclearrestantitumorPTP1BInhibitorinhibitorinhibit

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Pentamidine isethionate
Cat. No.:
HY-B0537B
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