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

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Acetazolamide sodium Chemical Structure

Acetazolamide sodium Chemical Structure

CAS No. : 1424-27-7

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Based on 5 publication(s) in Google Scholar

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Description

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

IC50 & Target

IC50: 30 nM (hCA IX), 130 nM (hCA II)[1]

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.

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

245.24

Formula

C4H6N4NaO3S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(NC1=NN=C(S(=O)(N)=O)S1)=O.[Na]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (407.76 mM)

DMSO : 100 mg/mL (407.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0776 mL 20.3882 mL 40.7764 mL
5 mM 0.8155 mL 4.0776 mL 8.1553 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.0776 mL 20.3882 mL 40.7764 mL 101.9410 mL
5 mM 0.8155 mL 4.0776 mL 8.1553 mL 20.3882 mL
10 mM 0.4078 mL 2.0388 mL 4.0776 mL 10.1941 mL
15 mM 0.2718 mL 1.3592 mL 2.7184 mL 6.7961 mL
20 mM 0.2039 mL 1.0194 mL 2.0388 mL 5.0970 mL
25 mM 0.1631 mL 0.8155 mL 1.6311 mL 4.0776 mL
30 mM 0.1359 mL 0.6796 mL 1.3592 mL 3.3980 mL
40 mM 0.1019 mL 0.5097 mL 1.0194 mL 2.5485 mL
50 mM 0.0816 mL 0.4078 mL 0.8155 mL 2.0388 mL
60 mM 0.0680 mL 0.3398 mL 0.6796 mL 1.6990 mL
80 mM 0.0510 mL 0.2549 mL 0.5097 mL 1.2743 mL
100 mM 0.0408 mL 0.2039 mL 0.4078 mL 1.0194 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • 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.

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Product Name:
Acetazolamide sodium
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HY-B0782A
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