1. Metabolic Enzyme/Protease
    Anti-infection
  2. Carbonic Anhydrase
    Bacterial
  3. Ethoxzolamide

Ethoxzolamide (Synonyms: Redupresin; L-643786; PNU-4191)

Cat. No.: HY-B1480 Purity: 99.43%
Handling Instructions

Ethoxzolamide is a carbonic anhydrase inhibitor with Ki of 1 nM.

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

Ethoxzolamide Chemical Structure

Ethoxzolamide Chemical Structure

CAS No. : 452-35-7

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10 mM * 1 mL in DMSO USD 106 In-stock
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100 mg USD 96 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Ethoxzolamide is a carbonic anhydrase inhibitor with Ki of 1 nM.

IC50 & Target

Ki: 1 nM (carbonic anhydrase)[1]

In Vitro

Ethoxzolamide (ETZ) treatment causes >90% inhibition of reporter GFP fluorescence in infected macrophages. Moreover, in a 9-day macrophage survival assay, Ethoxzolamide (ETZ) treatment significantly inhibits the ability of M. tuberculosis to grow intracellularly[2].

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

In Vivo

It is discovered that the lipid-soluble ethoxzolamide is converted in vivo to a water-soluble metabolite, while retaining high activity againstt the enzyme. At the minimal dose for maximal effect (4 mg/kg i.v. at 45 min) the IOP lowering is 4.2 mmHg, the concentration in anterior uvea is 2.5 pmol/kg, and the fractional inhibition of the enzyme (i) is 0.9995. The effect declines rapidly, attributable to the very short half-life of drug in plasma, leading to depletion of free drug in the anterior uvea and other tissues[1]. Ethoxzolamide (ETZ) strongly downregulates GFP reporter fluorescence in mouse lungs, with 3-fold inhibition of GFP signal compare to that in the mock-treating control. There is a significant reduction of bacterial survival in the lungs of ETZ-treating mice compare to the mock-treating control[2].

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

Molecular Weight

258.32

Formula

C₉H₁₀N₂O₃S₂

CAS No.

452-35-7

SMILES

O=S(C1=NC2=CC=C(OCC)C=C2S1)(N)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (387.12 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8712 mL 19.3558 mL 38.7117 mL
5 mM 0.7742 mL 3.8712 mL 7.7423 mL
10 mM 0.3871 mL 1.9356 mL 3.8712 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 (8.05 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (8.05 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (8.05 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

BMDMs are treated with 80 μM Ethoxzolamide (ETZ) or an equivalent volume of DMSO every 2 days for 9 days total. At days 3, 6, and 9, intracellular bacteria are quantified by lysing macrophage monolayers and performing serial dilution plating of lysates on 7H10 agar. For fluorescence microscopy experiments, macrophages are seeded on glass coverslips before infection with M. tuberculosis CDC1551. Samples are treated every 2 days with 100 μM Ethoxzolamide (ETZ) or an equal volume of DMSO for 9 days[2].

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

Animal Administration
[3]

Rats (male, 300–325 g) are randomly selected into 2 groups (n=6 each group) and Ethoxzolamide (EZ) is administered at a dose of 0.18 mg/kg (in PEG 300: ethanol, 1:1) via i.v. injection through the tail vein. Blood samples (about 50-100 µL) are collected in heparinizing tubes at 0, 15, 30, 60, 120, 180, 240, 360, 540, and 1440 min post-injection, via tail snip with isoflurane as anesthetic. Plasma samples are prepared and stored at -80 °C until analysis. To study the distribution in brain, rats in group 1 are scarified at 6 hours and rats in group 2 are scarified at 24 hours to collect the brain tissues. Those blood samples from group 2 are analyzed to generated PK profile[3].

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

References

Purity: 99.43%

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Keywords:

EthoxzolamideRedupresin L-643786 PNU-4191L643786L 643786L-643786PNU4191PNU 4191PNU-4191Carbonic AnhydraseBacterialCarbonate dehydrataseInhibitorinhibitorinhibit

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