An aldose reductase inhibitor
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AT-001

Item No. 36105

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7,8-dihydro-8-oxo-7-[[5-(trifluoromethyl)-2-benzothiazolyl]methyl]-pyrazino[2,3-d]pyridazine-5-acetic acid
CAS Number
1355612-71-3
Synonyms
  • Caficrestat
Molecular Formula
C17H10F3N5O3S
Formula Weight
421.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
221, 257 nm
SMILES
O=C(CC1=NN(CC2=NC3=C(S2)C=CC(C(F)(F)F)=C3)C(C4=NC=CN=C41)=O)O
InChi Code
InChI=1S/C17H10F3N5O3S/c18-17(19,20)8-1-2-11-9(5-8)23-12(29-11)7-25-16(28)15-14(21-3-4-22-15)10(24-25)6-13(26)27/h1-5H,6-7H2,(H,26,27)
InChi Key
YRGPAXAVTDMKDK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $35

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    5 mg

    $149

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    10 mg

    $228

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    25 mg

    $394

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    Product Description

    AT-001 is an inhibitor of aldose reductase (IC50 = 28.9 pM), the enzyme that converts glucose to sorbitol in the polyol pathway.1,2 AT-001 (40 mg/kg) reduces cardiac aldose reductase activity and sorbitol levels, diastolic function deficits, left ventricular hypertrophy, and cardiac fibrosis in a mouse model of diabetic cardiomyopathy.2 It also reduces mitochondrial fatty acid oxidation in isolated mouse hearts from the same model. AT-001 (0.2 nM) prevents senescence induced by high glucose, hydrogen peroxide, or mitomycin C (Item No. 11435) in primary normal human keratinocytes (NHK cells).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wasmuth, A., Landry, D., Deng, S.X., et al. Aldose reductase inhibitors and uses thereof. (2014).

    2. Gopal, K., Karwi, Q.G., Tabatabaei Dakhili, S.A., et al. Aldose reductase inhibition alleviates diabetic cardiomyopathy and is associated with a decrease in myocardial fatty acid oxidation. Cardiovasc. Diabetol. 22(1), 73 (2023).

    3. Yepuri, G., Kancharla, K., Perfetti, R., et al. The aldose reductase inhibitors AT-001, AT-003 and AT-007 attenuate human keratinocyte senescence. Front. Aging 5, 1466281 (2024).