| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
4-Hydroxymethylpyrazole targets alcohol dehydrogenase (ADH), the same enzyme as its parent compound, Fomepizole. However, it is a much weaker inhibitor, and its in vivo impact is considered negligible. As a metabolite, it is primarily relevant for its role in the pharmacokinetics and clearance of Fomepizole.
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|---|---|
| ln Vitro |
In vitro, 4-hydroxymethylpyrazole has a certain inhibitory effect on alcohol dehydrogenase, but its inhibition constant is significantly higher than that of Fomepizole. Its primary use is as an analytical standard for quantifying Fomepizole metabolism. It exhibits a plasma concentration that is positively correlated with the administered dosage of Fomepizole.
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| ln Vivo |
In vivo, 4-hydroxymethylpyrazole is the major circulating metabolite of Fomepizole. Its plasma concentration is directly related to the dose of Fomepizole administered. Its own in vivo impact on ADH inhibition is minimal due to its low potency.
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| Enzyme Assay |
Non-cellular assays for 4-hydroxymethylpyrazole are primarily analytical. It is measured in plasma and other biological samples using liquid chromatography-mass spectrometry (LC-MS) to monitor Fomepizole metabolism and pharmacokinetics. It can also be used as a reference standard in these assays.
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| Cell Assay |
4-Hydroxymethylpyrazole is not typically used in cellular assays as a pharmacological agent. Its role is as a metabolite. Its effects on ADH activity can be studied in cell lysates or tissue homogenates containing the enzyme.
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| Animal Protocol |
In vivo animal experiments with 4-hydroxymethylpyrazole are conducted to study the pharmacokinetics of Fomepizole. Animals are administered Fomepizole, and plasma levels of 4-hydroxymethylpyrazole are measured over time to determine the metabolic clearance and half-life of the parent drug.
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| ADME/Pharmacokinetics |
4-Hydroxymethylpyrazole has a relatively short half-life. Its plasma concentration correlates with Fomepizole dosage. It is formed in the liver and cleared renally. The compound is soluble in DMSO at 100 mg/mL and is typically stored as a powder at -20°C for up to 3 years or at 4°C for up to 2 years, and in solution at -80°C for 6 months or -20°C for 1 month.
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| Toxicity/Toxicokinetics |
4-Hydroxymethylpyrazole is considered to be of low toxicity, as it is the primary metabolite of Fomepizole, which is a clinically used drug. Its own pharmacological activity (ADH inhibition) is weak. It is not used as a therapeutic agent.
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| References | |
| Additional Infomation |
4-Hydroxymethylpyrazole is a type of pyrazole compound.
4-Hydroxymethylpyrazole is the primary metabolite of the alcohol dehydrogenase inhibitor Fomepizole. It is used as a reference standard and for studying Fomepizole pharmacokinetics. It has a certain inhibitory effect on alcohol dehydrogenase, but its impact is considered negligible in vivo. |
| Molecular Formula |
C₄H₆N₂O
|
|---|---|
| Molecular Weight |
98.10
|
| Exact Mass |
98.048
|
| CAS # |
25222-43-9
|
| PubChem CID |
3015210
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| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
326.8±17.0 °C at 760 mmHg
|
| Flash Point |
151.5±20.9 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
|
| Index of Refraction |
1.590
|
| LogP |
-0.87
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
7
|
| Complexity |
57.7
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JRMKJOOJKCAEJK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C4H6N2O/c7-3-4-1-5-6-2-4/h1-2,7H,3H2,(H,5,6)
|
| Chemical Name |
1H-pyrazol-4-ylmethanol
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| Synonyms |
4Hydroxymethylpyrazole; 4 Hydroxymethylpyrazole
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| 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) |
DMSO : ~100 mg/mL (~1019.37 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (25.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (25.48 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (25.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 10.1937 mL | 50.9684 mL | 101.9368 mL | |
| 5 mM | 2.0387 mL | 10.1937 mL | 20.3874 mL | |
| 10 mM | 1.0194 mL | 5.0968 mL | 10.1937 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.
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