Caficrestat (Synonyms: AT-001; Aldose reductase-IN-1)

Name: Caficrestat
Brand: MedChemExpress
SKU: HY-18967
Rating: 4.5 (0 reviews)

Cat. No.: HY-18967 Pureza: 99.74%: Ficha de datos
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Caficrestat (AT-001) is an orally active aldose reductase inhibitor. Caficrestat can be used in the study of diabetic cardiomyopathy.

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Caficrestat Estructura química

No. CAS : 1355612-71-3

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	Obtener un presupuesto
200 mg	Obtener un presupuesto

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Descripciòn

Caficrestat (AT-001) is an orally active aldose reductase inhibitor. Caficrestat can be used in the study of diabetic cardiomyopathy^[1]^[2].

In Vitro

Caficrestat (0.2 nM, 48 h) inhibits the activity of aldose reductase (AR) in normal human keratinocytes (NHK) (75%)^[1].
Caficrestat (0.2 nM, 48 h) inhibits high glucose (HG), hydrogen peroxide (H₂O₂), and mitomycin-c (MMC)-induced NHK senescence^[1].

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

RT-PCR^[1]

Cell Line:	NHK cells
Concentration:	0.2 nM
Incubation Time:	48 h
Result:	Down-regulated SA-β-galactosidase activity, γ-H2AX foci, CDKN1A, TP53, SASP, and SERPINE1 gene expression.

In Vivo

Caficrestat (40 mg/kg, p.o., 3 weeks) inhibits AR, myocardial fatty acid oxidation, cardiac fibrosis, and hypertrophy in diabetic cardiomyopathy (DbCM) mice^[2].

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

Animal Model:	Experimental type 2 DbCM model (8-week-old male C57BL/6J mice, high-fat diet [60% kcal from lard] for 10 weeks with a single intraperitoneal injection of Streptozotocin (HY-13753) (75 mg/kg) at 4 weeks)^[2]
Dosage:	40 mg/kg
Administration:	Oral gavage (p.o.), daily in light cycle for 3 weeks
Result:	Increased tissue Doppler e'/a' ratio and decreased E/e' ratio. Reduced LV mass. Reduced palmitate oxidation rate. Reduced cross-sectional collagen deposition. Reduced cardiomyocyte hypertrophy.

Ensayo clínico

Peso molecular

421.35

Fòrmula

C₁₇H₁₀F₃N₅O₃S

No. CAS

1355612-71-3

Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=NC=CN=C2C(CC(O)=O)=NN1CC3=NC4=C(C=CC(C(F)(F)F)=C4)S3

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : ≥ 28 mg/mL (66.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3733 mL	11.8666 mL	23.7332 mL
5 mM	0.4747 mL	2.3733 mL	4.7466 mL
10 mM	0.2373 mL	1.1867 mL	2.3733 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (5.93 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 (5.93 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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.

Pureza y Documentación

Purity: 99.74%

Select Batch:

Ficha de datos (276 KB) SDS (252 KB)

COA (251 KB) LCMS (93 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Yepuri G, Kancharla K, Perfetti R, Shendelman S, Wasmuth A, Ramasamy R. The aldose reductase inhibitors AT-001, AT-003 and AT-007 attenuate human keratinocyte senescence. Front Aging. 2024 Dec 17;5:1466281. [Content Brief]

[2]. Gopal K, et ak. Aldose reductase inhibition alleviates diabetic cardiomyopathy and is associated with a decrease in myocardial fatty acid oxidation. Cardiovasc Diabetol. 2023 Mar 28;22(1):73. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3733 mL	11.8666 mL	23.7332 mL	59.3331 mL
	5 mM	0.4747 mL	2.3733 mL	4.7466 mL	11.8666 mL
	10 mM	0.2373 mL	1.1867 mL	2.3733 mL	5.9333 mL
	15 mM	0.1582 mL	0.7911 mL	1.5822 mL	3.9555 mL
	20 mM	0.1187 mL	0.5933 mL	1.1867 mL	2.9667 mL
	25 mM	0.0949 mL	0.4747 mL	0.9493 mL	2.3733 mL
	30 mM	0.0791 mL	0.3956 mL	0.7911 mL	1.9778 mL
	40 mM	0.0593 mL	0.2967 mL	0.5933 mL	1.4833 mL
	50 mM	0.0475 mL	0.2373 mL	0.4747 mL	1.1867 mL
	60 mM	0.0396 mL	0.1978 mL	0.3956 mL	0.9889 mL

Caficrestat Related Classifications

Metabolic Disease

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:

Caficrestat1355612-71-3AT-001 Aldose reductase-IN-1AT001AT 001Aldose ReductaseDiabetic cardiomyopathyNHKARhigh glucoseInhibitorinhibitorinhibit

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Caficrestat (Synonyms: AT-001; Aldose reductase-IN-1)

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Complete Stock Solution Preparation Table

Caficrestat Related Classifications

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