| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg | |||
| Other Sizes |
| Targets |
Acetazolamide D3 targets carbonic anhydrase (CA), a family of zinc-containing metalloenzymes that catalyze the reversible hydration of carbon dioxide to bicarbonate and protons. Carbonic anhydrase is involved in various physiological processes including acid-base balance, fluid secretion, and electrolyte transport. By inhibiting carbonic anhydrase, Acetazolamide reduces bicarbonate formation, leading to diuresis (increased urine output), reduced intraocular pressure (in glaucoma), and decreased cerebrospinal fluid production (in epilepsy and altitude sickness). The deuterated D3 form is used as an analytical internal standard for quantifying Acetazolamide in biological samples.
|
|---|---|
| ln Vitro |
In vitro, Acetazolamide (parent compound) is a potent inhibitor of carbonic anhydrase. The compound binds to the active site zinc ion of carbonic anhydrase, blocking the enzyme's catalytic activity. In enzyme assays, Acetazolamide inhibits CA activity with IC₅0 values in the nanomolar range. The D3-labeled form is expected to exhibit identical in vitro enzyme inhibition activity to the parent compound, making it suitable as an internal standard for quantification. The compound is used in research to study carbonic anhydrase function and its role in various physiological and pathological processes.
|
| ln Vivo |
In vivo, Acetazolamide is clinically used as a diuretic, for the treatment of glaucoma, epilepsy, and altitude sickness. It is primarily used in both children and adults, although it may be used as monotherapy. As a carbonic anhydrase inhibitor, Acetazolamide reduces bicarbonate reabsorption in the kidney, leading to diuresis; reduces aqueous humor production in the eye, lowering intraocular pressure; and reduces cerebrospinal fluid production, decreasing intracranial pressure. The deuterated D3 form is used as an internal standard for pharmacokinetic studies and therapeutic drug monitoring, enabling accurate quantification of Acetazolamide levels in plasma and urine samples by LC-MS/MS.
|
| Enzyme Assay |
In vitro enzyme assays for Acetazolamide involve measuring carbonic anhydrase activity using isolated enzyme or tissue homogenates. The assay is performed in buffer containing the substrate p-nitrophenyl acetate or CO2. Varying concentrations of Acetazolamide or the D3 internal standard (0.001-100 microM) are incubated with the enzyme at 25degC for 5-10 minutes. Enzyme activity is measured spectrophotometrically by monitoring the change in absorbance at 348 nm (p-nitrophenyl acetate assay) or by pH change (CO2 hydration assay). IC₅0 values for CA inhibition are determined from dose-response curves. Ki values are calculated using the appropriate kinetic models.
|
| Cell Assay |
Cellular assays for Acetazolamide are performed using cells expressing carbonic anhydrase, such as renal epithelial cells (e.g., MDCK, LLC-PK1) or erythrocytes. Cells are cultured in appropriate medium and seeded in 6- or 96-well plates. Cells are treated with serial dilutions of Acetazolamide (0.001-100 microM) for 1-24 hours. Carbonic anhydrase activity in cell lysates is measured using a colorimetric or fluorometric CA assay kit. Intracellular pH is measured using fluorescent pH indicators (e.g., BCECF). Cell viability is assessed by MTT assay. IC₅0 values for CA inhibition in cells are calculated from dose-response curves.
|
| Animal Protocol |
In vivo animal studies for Acetazolamide are conducted in rodent models to study diuretic effects, intraocular pressure, and intracranial pressure. Rats or mice are administered Acetazolamide orally or intraperitoneally at doses of 10-100 mg/kg. Animals are placed in metabolic cages for urine collection over 24-hour periods. Urine volume, pH, and electrolyte excretion are measured. Intraocular pressure is measured using a tonometer. Intracranial pressure is measured using a pressure transducer. Pharmacokinetic parameters (Cmax, Tmax, AUC, t1/2) are determined from plasma and urine samples by LC-MS/MS using the D3 internal standard.
|
| ADME/Pharmacokinetics |
Acetazolamide D3 (CAS#: 1189904-01-5) has molecular formula C4H3D3N4O3S2 and molecular weight 225.26. The chemical name is N-(5-Sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide-2,2,2-d3. The compound is a deuterium-labeled form of Acetazolamide, a potent carbonic anhydrase inhibitor used as a diuretic, antiglaucoma, antiepileptic, and anti-altitude sickness agent. Purity is typically >98%. Storage should be at -20degC, protected from light and moisture. For research use only.
|
| Additional Infomation |
Acetazolamide D3 (CAS#: 1189904-01-5) is the deuterium-labeled form of Acetazolamide, a potent carbonic anhydrase (CA) inhibitor. Acetazolamide is used clinically as a diuretic, for the treatment of glaucoma, epilepsy, and altitude sickness. Carbonic anhydrase is a zinc-containing enzyme that catalyzes the hydration of carbon dioxide and is involved in acid-base balance, fluid secretion, and electrolyte transport. The D3-labeled analog is used as an internal standard in LC-MS/MS bioanalytical methods for pharmacokinetic studies, therapeutic drug monitoring, and clinical research. For research use only, not for human therapeutic applications.
|
| Molecular Formula |
C4H3D3N4O3S2
|
|---|---|
| Molecular Weight |
225.2639
|
| Exact Mass |
225.007
|
| CAS # |
1189904-01-5
|
| Related CAS # |
Acetazolamide;59-66-5;Acetazolamide sodium;1424-27-7
|
| PubChem CID |
46779906
|
| Appearance |
White to off-white solid powder
|
| LogP |
1.574
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
13
|
| Complexity |
297
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
[2H]C([2H])([2H])C(=O)NC1=NN=C(S1)S(=O)(=O)N
|
| InChi Key |
BZKPWHYZMXOIDC-FIBGUPNXSA-N
|
| InChi Code |
InChI=1S/C4H6N4O3S2/c1-2(9)6-3-7-8-4(12-3)13(5,10)11/h1H3,(H2,5,10,11)(H,6,7,9)/i1D3
|
| Chemical Name |
2,2,2-trideuterio-N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4393 mL | 22.1966 mL | 44.3931 mL | |
| 5 mM | 0.8879 mL | 4.4393 mL | 8.8786 mL | |
| 10 mM | 0.4439 mL | 2.2197 mL | 4.4393 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
