1. Metabolic Enzyme/Protease
  2. Aldose Reductase
  3. Tolrestat

Tolrestat (Synonyms: AY-27773)

Cat. No.: HY-16500 Purity: 98.85%
Handling Instructions

Tolrestat is a potent, orally active aldose reductase inhibitor with IC50 of 35 nM.

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

Tolrestat Chemical Structure

Tolrestat Chemical Structure

CAS No. : 82964-04-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 223 In-stock
Estimated Time of Arrival: December 31
5 mg USD 203 In-stock
Estimated Time of Arrival: December 31
10 mg USD 300 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1056 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1622 In-stock
Estimated Time of Arrival: December 31
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Description

Tolrestat is a potent, orally active aldose reductase inhibitor with IC50 of 35 nM.

IC50 & Target

IC50: 35 nM (Aldose Reductase)

In Vivo

Tolrestat (1.8 mg/kg per day) causes a reversal to normal RBC sorbitol levels diabetic rats[1]. In 21-day diabetic rats, the estimated ID in the sciatic nerve and lenses is 4.8 and about 20 for tolrestat, and 1.7 and 2.2 for (±)sorbinil, respectively[2]. Either tolrestat or sorbinil inhibits tissue AR activity but does not significantly affect plasma lipoprotein levels, or affect the body weight of the mice or their general health. Accumulation of cholesterol-rich foam cells is significantly increased in aortic roots of tolrestat-fed mice[3].

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

Molecular Weight

357.35

Formula

C₁₆H₁₄F₃NO₃S

CAS No.

82964-04-3

SMILES

O=C(O)CN(C(C1=C2C=CC(OC)=C(C(F)(F)F)C2=CC=C1)=S)C

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 (279.84 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7984 mL 13.9919 mL 27.9838 mL
5 mM 0.5597 mL 2.7984 mL 5.5968 mL
10 mM 0.2798 mL 1.3992 mL 2.7984 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (7.00 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (7.00 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.00 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

For a period of four days, rats weighing about 70 g are given unlimited access to water and Chow supplemented with 20% (wt/wt) galactose and tolrestat at various dose levels. Rats used as control receive chow containing galactose (20%, wt/wt) or glucose (20%, wt/wt). The rats are killed; the lenses and sciatic nerves are removed and homogenized in 5% trichloroacetic acid; the deproteinized extracts are then analyzed for galactitol by a modification of a method for glycerol determination. The values obtained in the group fed 20% glucose are used for background correction.

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

References

Purity: 98.85%

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Keywords:

TolrestatAY-27773AY27773AY 27773Aldose ReductaseInhibitorinhibitorinhibit

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Tolrestat
Cat. No.:
HY-16500
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