Fidarestat

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). It decreases sorbitol and myo-inositol levels in the sciatic nerve of rats with diabetes induced by streptozotocin (STZ, Cay-13104) when administered at a dose of 2 mg/kg per day. 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. Fidarestat (50 mg/kg per day) decreases metastasis in a KM20 human colorectal cancer mouse xenograft model.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: DMF: 3 mg/ml, DMSO: 5 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 1 mg/ml. lambdamax: 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.