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U-0521 is the inhibitor of the catechol-O-methyltransferase (COMT). U-0521 has the potential for the research of Parkinson's disease.

For research use only. We do not sell to patients.

U-0521 Chemical Structure

U-0521 Chemical Structure

CAS No. : 5466-89-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 231 In-stock
Solution
10 mM * 1 mL in DMSO USD 231 In-stock
Solid
5 mg USD 210 In-stock
10 mg USD 350 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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Description

U-0521 is the inhibitor of the catechol-O-methyltransferase (COMT). U-0521 has the potential for the research of Parkinson's disease[1].

IC50 & Target

COMT[1]

In Vitro

U-0521 inhibits RBC COMT activity in a dose-dependent manner with an IC50 of 6 x10-6 M[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

U-0521 (i.p.; 0-250 mg/kg; 10 min) inhibits COMT activity in a dose-dependent manner. 50% inhibition of enzyme activity is obtained at 90 mg/kg and maximum inhibition of 90% is obtained at 250 mg/kg[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (180-250 g)[1]
Dosage: 0-250 mg/kg
Administration: i.p.; 10 min
Result: Inhibited COMT activity in a dose-dependent manner. 50% inhibition of enzyme activity was obtained at 90mg/kg and maximum inhibition of 90% was obtained at 250 mg/kg.
Molecular Weight

180.20

Formula

C10H12O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C(C1=CC=C(C(O)=C1)O)=O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (554.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.5494 mL 27.7469 mL 55.4939 mL
5 mM 1.1099 mL 5.5494 mL 11.0988 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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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 (13.87 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 (13.87 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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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. 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 1 mM 5.5494 mL 27.7469 mL 55.4939 mL 138.7347 mL
5 mM 1.1099 mL 5.5494 mL 11.0988 mL 27.7469 mL
10 mM 0.5549 mL 2.7747 mL 5.5494 mL 13.8735 mL
15 mM 0.3700 mL 1.8498 mL 3.6996 mL 9.2490 mL
20 mM 0.2775 mL 1.3873 mL 2.7747 mL 6.9367 mL
25 mM 0.2220 mL 1.1099 mL 2.2198 mL 5.5494 mL
30 mM 0.1850 mL 0.9249 mL 1.8498 mL 4.6245 mL
40 mM 0.1387 mL 0.6937 mL 1.3873 mL 3.4684 mL
50 mM 0.1110 mL 0.5549 mL 1.1099 mL 2.7747 mL
60 mM 0.0925 mL 0.4624 mL 0.9249 mL 2.3122 mL
80 mM 0.0694 mL 0.3468 mL 0.6937 mL 1.7342 mL
100 mM 0.0555 mL 0.2775 mL 0.5549 mL 1.3873 mL
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U-0521 Related Classifications

Help & FAQs
  • 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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U-0521
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HY-121949
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