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

Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX. Acetazolamide has diuretic, antihypertensive and anti-gonococcal activities.

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

CAS No. : 59-66-5

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Based on 13 publication(s) in Google Scholar

Other Forms of Acetazolamide:

Acetazolamide Related Antibodies

Top Publications Citing Use of Products

    Acetazolamide purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2024 Apr 17;13(4):473.

    Effect of Acetazolamide, a CA inhibitor, on oxidation of PTEN by H2O2. HepG2 cells were pre-incubated in HCO3−-free media, supplemented with 0, 0.01, 0.1, 1, and 10 µM Acetazolamide, at 37 °C with 0.1% CO2 for 4 h. Then, they were changed to stimulation media with same components plus 0.5 mM H2O2. After 10 min, the reaction was terminated by NEM-containing lysis buffer. Western blot data with PTEN and β-actin antibodies are shown Acetazolamide considerably impeded PTEN oxidation in a dose-dependent manner.

    Acetazolamide purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2024 Apr 17;13(4):473.

    Effect of Acetazolamide, a CA inhibitor, on oxidation of PTEN by H2O2. HepG2 cells were pre-incubated in HCO3−-free media, supplemented with 0, 0.01, 0.1, 1, and 10 µM Acetazolamide, at 37 °C with 0.1% CO2 for 4 h. Then, they were changed to stimulation media with same components plus 0.5 mM H2O2. After 10 min, the reaction was terminated by NEM-containing lysis buffer. Western blot data with PTEN and β-actin antibodies are shown. Stars are considered as significances.

    Acetazolamide purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 May 17;42(5):112529.  [Abstract]

    GSIS was measured via static incubation in male human islets (n = 3–7 donors, 10 IEQ/condition measured in triplicate) cultured for 24 h with vehicle or DHT (10 nM) and then for 40 min in the presence or absence of a carbonic anhydrase inhibitor Acetazolamide (50 μM).

    Acetazolamide purchased from MedChemExpress. Usage Cited in: Elife. 2018 Feb 2;7:e33432.  [Abstract]

    Intracellular pH (pHi) of the ligated efferent ductules with or without Acetazolamide(500 μM) from WT mice and Adgrg2-/Y mice.

    View All Carbonic Anhydrase Isoform Specific Products:

    View All Isoforms
    CA CA I CA Ⅱ CA IX CA XII CA VII CA VI CA VA CA VB CA XIII CA XIV

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX. Acetazolamide has diuretic, antihypertensive and anti-gonococcal activities[1][4][5][6].

    IC50 & Target

    CA IX

     

    Cellular Effect
    Cell Line Type Value Description References
    HT-29 IC50
    53.78 μM
    Compound: AAZ
    Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 24 hrs under hypoxic condition by MTT assay
    Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 24 hrs under hypoxic condition by MTT assay
    		[PMID: 31542715]
    HT-29 IC50
    > 100 μM
    Compound: AAZ
    Cytotoxicity against human HT-29 cells after 96 hrs under hypoxic condition by MTT assay
    Cytotoxicity against human HT-29 cells after 96 hrs under hypoxic condition by MTT assay
    		[PMID: 29649740]
    HT-29 IC50
    > 100 μM
    Compound: AAZ
    Cytotoxicity against human HT-29 cells after 96 hrs under normoxic condition by MTT assay
    Cytotoxicity against human HT-29 cells after 96 hrs under normoxic condition by MTT assay
    		[PMID: 29649740]
    HeLa IC50
    2.83 μM
    Compound: AZA
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs under hypoxia condition by MTT assay
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs under hypoxia condition by MTT assay
    		[PMID: 31901743]
    HeLa IC50
    7.82 μM
    Compound: AZA
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs under normaxia condition by MTT assay
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs under normaxia condition by MTT assay
    		[PMID: 31901743]
    MDA-MB-231 IC50
    > 100 μM
    Compound: AAZ
    Cytotoxicity against human MDA-MB-231 cells after 96 hrs under hypoxic condition by MTT assay
    Cytotoxicity against human MDA-MB-231 cells after 96 hrs under hypoxic condition by MTT assay
    		[PMID: 29649740]
    MDA-MB-231 IC50
    > 100 μM
    Compound: AAZ
    Cytotoxicity against human MDA-MB-231 cells after 96 hrs under normoxic condition by MTT assay
    Cytotoxicity against human MDA-MB-231 cells after 96 hrs under normoxic condition by MTT assay
    		[PMID: 29649740]
    Oocyte IC50
    0.86 μM
    Compound: 1
    Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes
    Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes
    		[PMID: 18178093]
    Oocyte IC50
    0.9 μM
    Compound: 1
    Inhibition of human AQP4b-mediated water transport in Xenopus oocytes
    Inhibition of human AQP4b-mediated water transport in Xenopus oocytes
    		[PMID: 17178220]
    WI-38 IC50
    14.45 μM
    Compound: AZA
    Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    		[PMID: 31901743]
    In Vitro

    Acetazolamide also inhibits hCA II with an IC50 of 130 nM[1].
    Acetazolamide (Ace) is a small heteroaromatic sulfonamide that binds to various carbonic anhydrases with high affinity, acting as a carbonic anhydrase (CA) inhibitor[2].
    Compared with the control group, the high Acetazolamide concentration (AceH, 50 nM), Cisplatin (Cis; 1 μg/mL) and Cis combined with the low Acetazolamide concentration (AceL, 10 nM) treatments significantly reduces viability of Hep-2 cells[2].
    Treatment with the Acetazolamide/Cis combination significantly increases the expression levels of P53, as both AceL+Cis and AceH+Cis treatments result in significantly increased P53 protein expression levels compared with the control group. The Ace/Cis combination treatment significantly reduces the bcl-2/bax expression ratio, and increases the expression of caspase-3 protein, compared with the control group. AceL, AceH, Cis and AceL+Cis treatments significantly reduce the bcl-2/bax ratio compared with the control group[2].
    Combined Ace and Cis treatment effectively promotes apoptosis in Hep-2 cells[2].
    Combined treatment with Ace/Cis markedly decreases the expression of AQP1 mRNA in Hep-2 cells. Both AceH and AceL+Cis treatments decrease the expression of aquaporin-1 (AQP1) mRNA in Hep-2 cells compared with the control group[2].

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

    Acetazolamide Related Antibodies
    In Vivo

    Acetazolamide (40 mg/kg) significantly potentiates the inhibitory effect of MS-275 on tumorigenesis in neuroblastoma (NB) SH-SY5Y xenografts[3].
    Acetazolamide (40 mg/kg) and/or MS-275 treatment reduce expression of HIF1-α and CAIX in NB SH-SY5Y xenograft[3].
    Acetazolamide (40 mg/kg), MS-275 and Acetazolamide+MS-275 reduce expression of mitotic and proliferative markers in NB SH-SY5Y xenografts[3].
    Acetazolamide (50 mg/kg; PO, for 3 days) significantly reduces the gonococcal load in the vagina of infected mice by 90%[6].

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

    222.25

    Formula

    C4H6N4O3S2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(NC1=NN=C(S(=O)(N)=O)S1)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (224.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.4994 mL 22.4972 mL 44.9944 mL
    5 mM 0.8999 mL 4.4994 mL 8.9989 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Volume
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    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: ≥ 2.5 mg/mL (11.25 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (11.25 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 1.96 mg/mL (8.82 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
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    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%

    SDS (393 KB)

    COA (249 KB) HNMR (233 KB) RP-HPLC (247 KB) MS (229 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay

    Cell Viability Assay[2]
    Cell line: Hep-2 cells and HUVECs
    Concentration: 10 nM and 50 nM
    Incubation time: 48 h
    Assay: The cell viability of Hep-2 cells and HUVECs is measured by MTT assay. Hep-2 cells and HUVECs in logarithmic growth phase are plated in 96-well plates. Following 48 h of drug treatment as indicated, 200 µL MTT (5 mg/mL) is added to each well. Cells are incubated with the MTT solution at 37°C for 4 h. Then, 150 µL DMSO is added for 5 min. The optical density (OD) values are measured at 490 nm with a Versamax Microplate reader.
    Note: Combined treatment effectively reduced viability in Hep-2 cells.

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

    In vivo studies[3]
    Animal model: 4-6 weeks-old female NOD/SCID mice
    Dosage: 40 mg/kg, intraperitoneal injection, every day for 2 weeks
    Administration: Mice are randomized into four groups (5 mice per group). The control and treatment groups receive intraperitoneal injections of vehicle (PBS) or Acetazolamide (40 mg/kg), MS-275 (20 mg/kg) or the combination, respectively, every day for 2 weeks. Experiments are terminated when tumor sizes exceed 2 cm3 in volume or animals show signs of morbidity. Tumor diameters are measured on a daily basis until termination.
    Note: Inhibited tumor growth of NB xenografts with significant anti-tumor growth potentiation effect.

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.4994 mL 22.4972 mL 44.9944 mL 112.4859 mL
    5 mM 0.8999 mL 4.4994 mL 8.9989 mL 22.4972 mL
    10 mM 0.4499 mL 2.2497 mL 4.4994 mL 11.2486 mL
    15 mM 0.3000 mL 1.4998 mL 2.9996 mL 7.4991 mL
    20 mM 0.2250 mL 1.1249 mL 2.2497 mL 5.6243 mL
    25 mM 0.1800 mL 0.8999 mL 1.7998 mL 4.4994 mL
    30 mM 0.1500 mL 0.7499 mL 1.4998 mL 3.7495 mL
    40 mM 0.1125 mL 0.5624 mL 1.1249 mL 2.8121 mL
    50 mM 0.0900 mL 0.4499 mL 0.8999 mL 2.2497 mL
    60 mM 0.0750 mL 0.3750 mL 0.7499 mL 1.8748 mL
    80 mM 0.0562 mL 0.2812 mL 0.5624 mL 1.4061 mL
    100 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1249 mL
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    Acetazolamide 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:

    Acetazolamide59-66-5Carbonic AnhydraseAutophagyBacterialCarbonate dehydratasediureticantihypertensiveanti-gonococcalNeisseria gonorrhoeaeInhibitorinhibitorinhibit

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