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

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

Cat. No.: HY-B1480 Purity: 99.85%
COA Handling Instructions

Molarity Calculator

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

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Ethoxzolamide Chemical Structure

Ethoxzolamide Chemical Structure

CAS No. : 452-35-7

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Based on 1 publication(s) in Google Scholar

Ethoxzolamide Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

Ethoxzolamide Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

258.32

Formula

C9H10N2O3S2
CAS No.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (387.12 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.85%

COA (246 KB) HNMR (133 KB) RP-HPLC (168 KB) LCMS (382 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.8712 mL 19.3558 mL 38.7117 mL 96.7792 mL
5 mM 0.7742 mL 3.8712 mL 7.7423 mL 19.3558 mL
10 mM 0.3871 mL 1.9356 mL 3.8712 mL 9.6779 mL
15 mM 0.2581 mL 1.2904 mL 2.5808 mL 6.4519 mL
20 mM 0.1936 mL 0.9678 mL 1.9356 mL 4.8390 mL
25 mM 0.1548 mL 0.7742 mL 1.5485 mL 3.8712 mL
30 mM 0.1290 mL 0.6452 mL 1.2904 mL 3.2260 mL
40 mM 0.0968 mL 0.4839 mL 0.9678 mL 2.4195 mL
50 mM 0.0774 mL 0.3871 mL 0.7742 mL 1.9356 mL
60 mM 0.0645 mL 0.3226 mL 0.6452 mL 1.6130 mL
80 mM 0.0484 mL 0.2419 mL 0.4839 mL 1.2097 mL
100 mM 0.0387 mL 0.1936 mL 0.3871 mL 0.9678 mL
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Ethoxzolamide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ethoxzolamide452-35-7Redupresin L-643786 PNU-4191L643786L 643786L-643786PNU4191PNU 4191PNU-4191Carbonic AnhydraseBacterialCarbonate dehydrataseInhibitorinhibitorinhibit

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