1. Metabolic Enzyme/Protease
  2. Drug Metabolite
  3. 4-Hydroxymethylpyrazole

4-Hydroxymethylpyrazole is the primary metabolite of Fomepizole (HY-B0876) produced through hepatic oxidative metabolism. 4-Hydroxymethylpyrazole exhibits a plasma concentration that is positively correlated with the administered dosage of Fomepizole, and it demonstrates a relatively short half-life. 4-Hydroxymethylpyrazole demonstrates inhibitory effects on alcohol dehydrogenase (ADH) in both humans and monkeys, but its inhibition constant is significantly higher than that of Fomepizole, rendering its in vivo impact negligible.

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4-Hydroxymethylpyrazole

4-Hydroxymethylpyrazole Chemical Structure

CAS No. : 25222-43-9

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of 4-Hydroxymethylpyrazole:

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  • Purity & Documentation

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Description

4-Hydroxymethylpyrazole is the primary metabolite of Fomepizole (HY-B0876) produced through hepatic oxidative metabolism. 4-Hydroxymethylpyrazole exhibits a plasma concentration that is positively correlated with the administered dosage of Fomepizole, and it demonstrates a relatively short half-life. 4-Hydroxymethylpyrazole demonstrates inhibitory effects on alcohol dehydrogenase (ADH) in both humans and monkeys, but its inhibition constant is significantly higher than that of Fomepizole, rendering its in vivo impact negligible[1].

Molecular Weight

98.11

Formula

C4H6N2O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OCC1=CNN=C1

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

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 : 100 mg/mL (1019.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (1019.26 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 10.1926 mL 50.9632 mL 101.9264 mL
5 mM 2.0385 mL 10.1926 mL 20.3853 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. 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (25.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (25.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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

Purity: 99.74%

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. 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
DMSO / H2O 1 mM 10.1926 mL 50.9632 mL 101.9264 mL 254.8160 mL
5 mM 2.0385 mL 10.1926 mL 20.3853 mL 50.9632 mL
10 mM 1.0193 mL 5.0963 mL 10.1926 mL 25.4816 mL
15 mM 0.6795 mL 3.3975 mL 6.7951 mL 16.9877 mL
20 mM 0.5096 mL 2.5482 mL 5.0963 mL 12.7408 mL
25 mM 0.4077 mL 2.0385 mL 4.0771 mL 10.1926 mL
30 mM 0.3398 mL 1.6988 mL 3.3975 mL 8.4939 mL
40 mM 0.2548 mL 1.2741 mL 2.5482 mL 6.3704 mL
50 mM 0.2039 mL 1.0193 mL 2.0385 mL 5.0963 mL
60 mM 0.1699 mL 0.8494 mL 1.6988 mL 4.2469 mL
80 mM 0.1274 mL 0.6370 mL 1.2741 mL 3.1852 mL
100 mM 0.1019 mL 0.5096 mL 1.0193 mL 2.5482 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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Product Name:
4-Hydroxymethylpyrazole
Cat. No.:
HY-33914
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