| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| Other Sizes |
| Targets |
Allopurinol sodium targets xanthine oxidase, a key enzyme in the purine metabolism pathway that catalyzes the oxidation of hypoxanthine to xanthine and xanthine to uric acid. By inhibiting xanthine oxidase, allopurinol sodium reduces the production of uric acid, the end product of purine metabolism. This mechanism is the basis for its use in the treatment of gout and hyperuricemia. The compound is a structural isomer of hypoxanthine, allowing it to competitively inhibit xanthine oxidase. Its sodium salt form offers improved aqueous solubility for research and pharmaceutical applications.
|
|---|---|
| ln Vitro |
In HFF and HUVEC cells, allopurinol sodium (0, 10, 100, 1000 µg/ml; 17 hours) can decrease HIF-1α and HIF-2α protein expression [5]. HUVEC cells' angiogenic characteristics can be diminished by allopurinol sodium (0, 10, 100, or 1000 µg/ml; 24 hours) [5].
In vitro, allopurinol sodium demonstrates potent inhibition of xanthine oxidase with an IC50 of 7.82 ± 0.12 μM. The compound inhibits the conversion of xanthine to uric acid, as measured by enzyme activity assays using purified xanthine oxidase or cell lysates. Its activity is concentration-dependent, with effective concentrations in the micromolar range. In cell-based assays, allopurinol sodium reduces uric acid production and may modulate oxidative stress. It has also been studied for its effects on cell viability and signaling pathways. |
| ln Vivo |
Allopurinol sodium (39 mg/kg; oral; daily for 21 days) showed antidepressant effect in rats [3]. Allopurinol sodium (10-400 mg/kg; i.p.) causes antinociceptive action in mice [4].
In vivo, allopurinol sodium has been studied in animal models for its effects on uric acid levels, gout, and other conditions. Oral administration of allopurinol sodium (39 mg/kg; daily for 21 days) showed antidepressant effects in rats. Intraperitoneal administration (10-400 mg/kg) caused antinociceptive action in mice. The compound is effective in reducing serum and urinary uric acid levels, making it a valuable tool for studying hyperuricemia and gout. Its in vivo effects are dose-dependent and mediated through xanthine oxidase inhibition. |
| Enzyme Assay |
The in vitro xanthine oxidase inhibition assay for allopurinol sodium typically uses purified xanthine oxidase enzyme and measures the conversion of xanthine to uric acid. The assay is performed in 96-well plates with xanthine as the substrate, varying concentrations of the test compound (typically 0.1 to 100 µM), and the enzyme in assay buffer. The reaction is initiated by adding xanthine, and the production of uric acid is monitored by measuring absorbance at 290 nm over time. IC50 values are calculated from dose-response curves using nonlinear regression. Positive controls (e.g., allopurinol) and negative controls (buffer) are included in each assay run.
|
| Cell Assay |
Western Blot Analysis[5]
Cell Types: HFF, HUVEC Cell Tested Concentrations: 0, 10, 100, 1000 µg/ml Incubation Duration: 17 hrs (hours) Experimental Results: HIF-1α and HIF-2α protein expression diminished in a dose-dependent manner. For in vitro cellular assays, cells (e.g., hepatocytes, renal cells) are treated with allopurinol sodium at concentrations ranging from 0.1 to 100 µM for 24-72 hours. Uric acid levels in the culture medium are measured by colorimetric or enzymatic assays. Cell viability is assessed using MTT or CellTiter-Glo assays. Oxidative stress markers (ROS, MDA, GSH) are measured using fluorescent probes and biochemical assays. For mechanism studies, the effects of the compound on xanthine oxidase activity and downstream signaling pathways are investigated. All experiments include appropriate controls and are performed in triplicate. |
| Animal Protocol |
Animal/Disease Models: 20-30 g, male Swiss albino mouse [3]
Doses: 39 mg/kg Route of Administration: oral; one time/day for 21 days Experimental Results: diminished immobility time in FST, immobility time was 129.8± 10.5 seconds. Animal/Disease Models: 30-40 g, male adult Swiss albino mouse [4] Doses: 10, 50, 100, 200, 400 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Dose dependence in tail flick and thermal stimulation Sexual antinociceptive effects plate. For in vivo efficacy studies, rodent models of hyperuricemia or gout are used. Allopurinol sodium is administered orally or intraperitoneally at doses ranging from 10 to 400 mg/kg. Serum and urinary uric acid levels are measured using colorimetric or enzymatic assays. In antidepressant studies, behavioral tests such as the forced swim test or tail suspension test are performed. In antinociceptive studies, pain behaviors are assessed using the hot plate test or acetic acid-induced writhing test. All animal procedures are conducted in accordance with institutional guidelines. |
| ADME/Pharmacokinetics |
The pharmacokinetic properties of allopurinol sodium are consistent with those of allopurinol. Following oral administration, allopurinol is rapidly absorbed and extensively metabolized to its active metabolite, oxypurinol. The plasma half-life of allopurinol is approximately 1-2 hours, while oxypurinol has a longer half-life of approximately 18-30 hours. The compound is eliminated primarily via renal excretion. The sodium salt form offers improved aqueous solubility compared to the parent compound.
|
| Toxicity/Toxicokinetics |
The toxicology of allopurinol sodium has been extensively evaluated. In therapeutic doses, the compound is generally well-tolerated. Adverse effects include gastrointestinal disturbances, skin rashes, and hypersensitivity reactions. In rare cases, severe adverse effects such as Stevens-Johnson syndrome and hepatotoxicity may occur. The compound is not genotoxic or carcinogenic. Allopurinol sodium is approved for clinical use in the treatment of gout and hyperuricemia.
|
| References | |
| Additional Infomation |
Allopurinol Sodium is the sodium salt of allopurine, a structural isomer of hypoxanthine. Allopurine inhibits xanthine oxidase, an enzyme that converts oxypurine into uric acid. By blocking uric acid production, this drug reduces the concentration of uric acid in serum and urine, thereby protecting the body from uric acid-mediated end-organ damage in diseases associated with excessive uric acid production, such as the massive cell lysis that occurs during the treatment of certain malignant tumors. (NCI04)
See also: Allopurinol Sodium (preferred); Allopurine (containing the active fraction). Allopurinol sodium is a xanthine oxidase inhibitor used in research related to gout and hyperuricemia. It has a molecular formula of C5H3N4NaO and a molecular weight of 158.09. The compound is approved for clinical use and is available as a pharmaceutical-grade compound for research and medicinal use. Its xanthine oxidase inhibition makes it a valuable tool for studying purine metabolism, oxidative stress, and related diseases. |
| Molecular Formula |
C5H3N4O-.NA+
|
|---|---|
| Molecular Weight |
158.09332
|
| Exact Mass |
158.02
|
| CAS # |
17795-21-0
|
| Related CAS # |
Allopurinol;315-30-0
|
| PubChem CID |
135566116
|
| Appearance |
White to off-white solid powder
|
| LogP |
0.496
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
11
|
| Complexity |
195
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
PTJRZVJXXNYNLN-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C5H4N4O.Na/c10-5-3-1-8-9-4(3)6-2-7-5;/h1-2H,(H2,6,7,8,9,10);/q;+1/p-1
|
| Chemical Name |
sodium;5H-pyrazolo[3,4-d]pyrimidin-1-id-4-one
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~50 mg/mL (~314.27 mM)
|
|---|---|
| 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 | 6.3255 mL | 31.6276 mL | 63.2551 mL | |
| 5 mM | 1.2651 mL | 6.3255 mL | 12.6510 mL | |
| 10 mM | 0.6326 mL | 3.1628 mL | 6.3255 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
