2. Metabolic Enzyme/Protease
  3. Aldose Reductase
  4. Zopolrestat

Zopolrestat  (Synonyms: CP73850)

Cat. No.: HY-19687 Purity: 99.92%
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Zopolrestat (CP73850) is a potent, orally active aldose reductase (AR) inhibitor with an IC50 of 3.1 nM. Zopolrestat is used for the research of diabetic complications.

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

Zopolrestat Chemical Structure

Zopolrestat Chemical Structure

CAS No. : 110703-94-1

Size Price Stock Quantity
1 mg USD 38 In-stock
5 mg USD 76 In-stock
10 mg USD 115 In-stock
25 mg USD 253 In-stock
50 mg USD 380 In-stock
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This product is a controlled substance and not for sale in your territory.

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Based on 1 publication(s) in Google Scholar

Zopolrestat Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Zopolrestat

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Zopolrestat (CP73850) is a potent, orally active aldose reductase (AR) inhibitor with an IC50 of 3.1 nM. Zopolrestat is used for the research of diabetic complications[1].

In Vitro

Zopolrestat is a potent inhibitor of the reduction of both glyceraldehyde and glucose by the human and rat enzymes[1].

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

Zopolrestat Related Antibodies
In Vivo

Zopolrestat (2.5 mg/kg-50 mg/kg; p.o.; once-a-day for 5 days) and left untreated for 7 days) prevents accumulation of sorbitol in the kidney cortex of diabetic rats and normalize elevated renal blood flow in galactosemic rats[1].

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

Animal Model: Male Sprague-Dawley rats (made diabetic by iv injection of streptozotocin)[1].
Dosage: 2.5 mg/kg-50 mg/kg
Administration: P.o.; once-a-day for 5 days
Result: Its ED50s in reversing already elevated sorbitol accumulation in rat sciatic nerve, retina, and lens in a chronic test were 1.9, 17.6, and 18.4 mg/kg, respectively.
Molecular Weight

419.38

Formula

C19H12F3N3O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CC1=NN(CC2=NC3=CC(C(F)(F)F)=CC=C3S2)C(C4=C1C=CC=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (238.45 mM; ultrasonic and warming and heat to 60°C; 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 2.3845 mL 11.9224 mL 23.8447 mL
5 mM 0.4769 mL 2.3845 mL 4.7689 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 (protect from light). 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
=
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: ≥ 0.83 mg/mL (1.98 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (1.98 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 20 mg/mL (47.69 mM); Suspended solution; Need ultrasonic

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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 (protect from light). 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 2.3845 mL 11.9224 mL 23.8447 mL 59.6118 mL
5 mM 0.4769 mL 2.3845 mL 4.7689 mL 11.9224 mL
10 mM 0.2384 mL 1.1922 mL 2.3845 mL 5.9612 mL
15 mM 0.1590 mL 0.7948 mL 1.5896 mL 3.9741 mL
20 mM 0.1192 mL 0.5961 mL 1.1922 mL 2.9806 mL
25 mM 0.0954 mL 0.4769 mL 0.9538 mL 2.3845 mL
30 mM 0.0795 mL 0.3974 mL 0.7948 mL 1.9871 mL
40 mM 0.0596 mL 0.2981 mL 0.5961 mL 1.4903 mL
50 mM 0.0477 mL 0.2384 mL 0.4769 mL 1.1922 mL
60 mM 0.0397 mL 0.1987 mL 0.3974 mL 0.9935 mL
80 mM 0.0298 mL 0.1490 mL 0.2981 mL 0.7451 mL
100 mM 0.0238 mL 0.1192 mL 0.2384 mL 0.5961 mL
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Zopolrestat 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.

Keywords:

Zopolrestat110703-94-1CP73850CP 73850CP-73850Aldose ReductasepotentoralaldosediabeticratsglyceraldehydeglucoseInhibitorinhibitorinhibit

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