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Aldose reductase-IN-1

Aldose reductase-IN-1
Aldose reductase-IN-1 (AT-001, Caficrestat) is a highly potent inhibitor of aldose reductase with an IC50 value of 28.9 pM, which can target the relaxin hormone signaling pathway in prostate cancer models.
Catalog No. T14175Cas No. 1355612-71-3
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Purity:99.82%
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Aldose reductase-IN-1

Purity: 99.82%
Catalog No. T14175Alias Caficrestat, AT-001Cas No. 1355612-71-3

Aldose reductase-IN-1 (AT-001, Caficrestat) is a highly potent inhibitor of aldose reductase with an IC50 value of 28.9 pM, which can target the relaxin hormone signaling pathway in prostate cancer models.
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Pack SizePriceAvailabilityQuantity
1 mg$52In Stock
5 mg$123In Stock
10 mg$187In Stock
25 mg$357In Stock
50 mg$538In Stock
100 mg$766In Stock
1 mL x 10 mM (in DMSO)$135In Stock
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Product Introduction

Bioactivity
Description
Aldose reductase-IN-1 (AT-001, Caficrestat) is a highly potent inhibitor of aldose reductase with an IC50 value of 28.9 pM, which can target the relaxin hormone signaling pathway in prostate cancer models.
In vitro
METHODS: To confirm that Aldose reductase-IN-1( AT-001,Caficrestat) retains its ability to bind to the major relaxin receptor RXFP1, H2 relaxin was labeled with 125I using Pierce iodination reagent, which radioiodinates the phenol aromatic ring of the Tyr residue (Tyr3 on the A chain).
RESULTS In an in vitro cell assay using the 293T.RXFP1 cell line, we showed that H2 relaxin binds to RXFP1 in the presence of a cognate competitive RBA with a Kd of 17.0 nM; similarly, Aldose reductase-IN-1( AT-001,Caficrestat) was shown to retain its binding ability to RXFP1 in the presence of a competitive RBA, inhibiting the binding of 125I-labeled H2 relaxin with a Ki of 9.2 μM[3].
In vivo
METHODS: Male C57BL/6J mice (8 weeks old) were subjected to experimental type 2 diabetes/diabetic cardiomyopathy for 10 weeks. At 4 weeks, they were given a single intraperitoneal injection of streptozotocin (75 mg/kg). Animals were then randomly assigned to Aldose reductase-IN-1 (AT-001, Caficrestat) (40 mg/kg/day, intraperitoneal injection, for 3 weeks). At the completion of the study, hearts were perfused in an isolated working mode to assess energy metabolism.
RESULTS Aldose reductase-IN-1 (AT-001, Caficrestat) improved diastolic function and cardiac efficiency in mice with experimental type 2 diabetes; in mice with diabetic cardiomyopathy, Aldose reductase-IN-1 (AT-001, Caficrestat) also reduced cardiac fibrosis and hypertrophy. [1]
AliasCaficrestat, AT-001
Chemical Properties
Molecular Weight421.35
FormulaC17H10F3N5O3S
Cas No.1355612-71-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 45 mg/mL (106.8 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3733 mL11.8666 mL23.7332 mL118.6662 mL
5 mM0.4747 mL2.3733 mL4.7466 mL23.7332 mL
10 mM0.2373 mL1.1867 mL2.3733 mL11.8666 mL
20 mM0.1187 mL0.5933 mL1.1867 mL5.9333 mL
50 mM0.0475 mL0.2373 mL0.4747 mL2.3733 mL
100 mM0.0237 mL0.1187 mL0.2373 mL1.1867 mL

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