An aldose reductase inhibitor
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Fidarestat

Item No. 21756

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S,4S)-6-fluoro-2,3-dihydro-2',5'-dioxo-spiro[4H-1-benzopyran-4,4'-imidazolidine]-2-carboxamide
CAS Number
136087-85-9
Molecular Formula
C12H10FN3O4
Formula Weight
279.2
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 1 mg/ml
λmax
204, 283 nm
SMILES
NC([C@H](C[C@]12N([H])C(N([H])C2=O)=O)OC3=C1C=C(F)C=C3)=O
InChi Code
InChI=1S/C12H10FN3O4/c13-5-1-2-7-6(3-5)12(4-8(20-7)9(14)17)10(18)15-11(19)16-12/h1-3,8H,4H2,(H2,14,17)(H2,15,16,18,19)/t8-,12-/m0/s1
InChi Key
WAAPEIZFCHNLKK-UFBFGSQYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    Fidarestat is an aldose reductase inhibitor (IC50 = 0.026 μM using human recombinant enzyme) that also inhibits aldo-keto reductase family 1 member B10 (AKR1B10; IC50 = 33 μM using human recombinant enzyme).1 It decreases sorbitol and myo-inositol levels in the sciatic nerve of rats with diabetes induced by streptozotocin (STZ; Item No. 13104) when administered at a dose of 2 mg/kg per day.2 Fidarestat (2 mg/kg per day) decreases nerve fiber abnormalities and reverses slowing of motor nerve conduction velocity (MNCV) in an STZ-induced diabetic rat model of peripheral neuropathy. It decreases the pain threshold in STZ-induced diabetic mice that overexpress human aldose reductase when administered at 4 mg/kg per day.3 Fidarestat (50 mg/kg per day) decreases metastasis in a KM20 human colorectal cancer mouse xenograft model.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ruiz, F.X., Cousido-Siah, A., Mitschler, A., et al. X-ray structure of the V301L aldo-keto reductase 1B10 complexed with NADP+ and the potent aldose reductase inhibitor fidarestat: Implications for inhibitor binding and selectivity. Chem. Biol. Interact. 202(1-3), 178-185 (2013).

    2. Kato, N., Mizuno, K., Matsubara, A., et al. Effect of long-term treatment with a new aldose reductase inhibitor, (2S,4S)-6-fluoro-2',5'-dioxospiro-[chroman-4,4'-imidazolidine]-2-carbox amide (SNK-860), on peripheral neuropathy in streptozotocin-induced diabetic rats. J. Diabetes Complications 8(1), 27-32 (1994).

    3. Uehara, K., Yamagishi, S., Otsuki, S., et al. Effects of polyol pathway hyperactivity on protein kinase C activity, nociceptive peptide expression, and neuronal structure in dorsal root ganglia in diabetic mice. Diabetes 53(12), 3239-3247 (2004).

    4. Tammali, R., Reddy, A.B., Saxena, A., et al. Inhibition of aldose reductase prevents colon cancer metastasis. Carcinogenesis 32(8), 1259-1267 (2011).