Art. -Nr.: HY-19687

Zopolrestat

(Synonyms: CP73850)

1 Cited Publications

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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.

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Reinheit: 99.92%
CAS. Nr.: 110703-94-1
Formel: C₁₉H₁₂F₃N₃O₃S
Molecular Weight:419.38

Speicherung:

4°C, protect from light

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

Zopolrestat Chemical Structure

CAS. Nr.: 110703-94-1

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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.

Chemical Information

CAS. Nr. 110703-94-1
Appearance Solid
Molecular Weight 419.38
Formel C₁₉H₁₂F₃N₃O₃S
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
Synonyms

CP73850
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

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

Publications (1)

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Journal Impact Factor

Patent

US20240216332A1.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3845 mL

11.9224 mL

23.8447 mL

5 mM

0.4769 mL

2.3845 mL

4.7689 mL

10 mM

0.2384 mL

1.1922 mL

2.3845 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.83 mg/mL (1.98 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mylari BL, et al. Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl] methyl]-1-phthalazineacetic acid (zopolrestat) and congeners. J Med Chem. 1991;34(1):108-122. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Zopolrestat

1 Cited Publications

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Zopolrestat

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Mass Spectrometry Human Metabolite Library

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Publications Citing Use of MedChemExpress (MCE) Zopolrestat

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zopolrestat

Metabolism/Protease Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Orally Active Compound Library

Glucose Metabolism Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Zopolrestat

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zopolrestat Related Classifications

HY-19687 Related Classifications