1. Metabolic Enzyme/Protease
    Autophagy
  2. Carbonic Anhydrase
    Autophagy
  3. Acetazolamide

Acetazolamide 

Cat. No.: HY-B0782 Purity: 99.87%
Handling Instructions

Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX. Diuretic effects.

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

Acetazolamide Chemical Structure

Acetazolamide Chemical Structure

CAS No. : 59-66-5

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Description

Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX[1]. Diuretic effects[4].

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].

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].

Clinical Trial
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 : ≥ 41 mg/mL (184.48 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.4499 mL 2.2497 mL 4.4994 mL
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

222.25

Formula

C₄H₆N₄O₃S₂

CAS No.

59-66-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.87%

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Acetazolamide
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Acetazolamide

Cat. No.: HY-B0782