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Caficrestat

Cat. No. M28233
Caficrestat Structure
Synonym:

Aldose reductase-IN-1; AT-001

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Biological Activity

Caficrestat (Aldose reductase-IN-1) is a inhibitor of aldose reductase with IC50 of 28.9 pM.

Chemical Information
Molecular Weight 421.35
Formula C17H10F3N5O3S
CAS Number 1355612-71-3
Form Solid
Solubility (25°C) DMSO ≥ 28 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Keshav Gopal, et al. Cardiovasc Diabetol. Aldose reductase inhibition alleviates diabetic cardiomyopathy and is associated with a decrease in myocardial fatty acid oxidation

[2] James L Januzzi Jr, et al. Am Heart J. Rationale and design of the Aldose Reductase Inhibition for Stabilization of Exercise Capacity in Heart Failure Trial (ARISE-HF) in patients with high-risk diabetic cardiomyopathy

[3] Juan Gaztanaga, et al. Diabetes Metab Syndr. A pilot open-label study of aldose reductase inhibition with AT-001 (caficrestat) in patients hospitalized for COVID-19 infection: Results from a registry-based matched-control analysis

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Abmole Inhibitor Catalog




Keywords: Caficrestat, Aldose reductase-IN-1; AT-001 supplier, Aldose Reductase, inhibitors, activators


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