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

Risarestat (CT-112), an aldose reductase inhibitor, is developed for the treatment of diabetic complications.

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Risarestat Chemical Structure

Risarestat Chemical Structure

CAS No. : 79714-31-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 473 In-stock
Solution
10 mM * 1 mL in DMSO USD 473 In-stock
Solid
1 mg USD 172 In-stock
5 mg USD 430 In-stock
10 mg USD 700 In-stock
25 mg USD 1400 In-stock
50 mg USD 2300 In-stock
100 mg USD 3680 In-stock
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Risarestat Related Antibodies

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Description

Risarestat (CT-112), an aldose reductase inhibitor, is developed for the treatment of diabetic complications.

In Vivo

Risarestat inhibits the accumulation of dulcitol in a dose-dependent manner, except for the 1.0% solution which has an activity comparable to the 0.25% solution[1]. Risarestat peaks in the corneal epithelium, stroma, endothelium and aqueous humor in 30 minutes following instillation, then gradually diminishes time-dependently over a period of 24 hours. Risarestat remains detectable in the lens up to 24 hours, with a peak concentration at 2 hours after instillation[2]. The anterior surface area of superficial cells in the group treated with Risarestat is significantly decreases from a mean value of 881 to 728 microns2. Corneal sensitivity significantly improves from 5.36 to 1.37 g/mm2[3]. Animals treated with Risarestat shows a significant increase in the mean blinkresponse compared to untreated galactose-fed rats and does not differ significantly from controls towards the completion of the 7 month study. Animals treated topically with Risarestat and untreated galactose-fed rats develop bilateral nuclear cataracts within 3 weeks[4].

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

323.41

Formula

C16H21NO4S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(N1)SC(C2=CC=C(OCCCCC)C(OCC)=C2)C1=O
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 : 105 mg/mL (324.67 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 3.0921 mL 15.4603 mL 30.9205 mL
5 mM 0.6184 mL 3.0921 mL 6.1841 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% Corn Oil

    Solubility: ≥ 5.25 mg/mL (16.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.25 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 (52.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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(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:
%
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% 
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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
Animal Administration
[1][2]

Rats: The other 5 groups are fed on a 50% galactose diet, and 0.1, 0.25, 0.5 or 1.0% Risarestat ophthalmic solution or its vehicle is instilled in both eyes 4 times a day in each of the 5 treated groups. After 2 weeks, the corneal epithelium is scraped off in all rats and its dulcitol content is determined by gas chromatography[1].

Rabbits: Risarestat is prepared in acetate-buffered saline. 50 μL of 0.5% Risarestat in 7mM acetate-buffered saline (pH 5.2, 290 mOsm) containing 0.15% chlorbutanol as a preservative is instilled to both conjunctival sac of rabbits. This ophthalmic solution is proven to be untoxic to the external eye after 90 days' instillation to the rabbits 9 times a day. The rabbits are then sacrificed at, 15 and 30 minutes, 1, 2, 4, 8, and 24 hours after instillation[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 3.0921 mL 15.4603 mL 30.9205 mL 77.3013 mL
5 mM 0.6184 mL 3.0921 mL 6.1841 mL 15.4603 mL
10 mM 0.3092 mL 1.5460 mL 3.0921 mL 7.7301 mL
15 mM 0.2061 mL 1.0307 mL 2.0614 mL 5.1534 mL
20 mM 0.1546 mL 0.7730 mL 1.5460 mL 3.8651 mL
25 mM 0.1237 mL 0.6184 mL 1.2368 mL 3.0921 mL
30 mM 0.1031 mL 0.5153 mL 1.0307 mL 2.5767 mL
40 mM 0.0773 mL 0.3865 mL 0.7730 mL 1.9325 mL
50 mM 0.0618 mL 0.3092 mL 0.6184 mL 1.5460 mL
60 mM 0.0515 mL 0.2577 mL 0.5153 mL 1.2884 mL
80 mM 0.0387 mL 0.1933 mL 0.3865 mL 0.9663 mL
100 mM 0.0309 mL 0.1546 mL 0.3092 mL 0.7730 mL
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Risarestat Related Classifications

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  • 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:

Risarestat79714-31-1CT 112CT112CT-112Aldose ReductaseInhibitorinhibitorinhibit

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