ARI-809
ARI-809 (CP-744809) is a highly selective, orally active aldose reductase inhibitor with an IC50 of 1 nM. ARI-809 blocks excessive glucose flux through the polyol pathway. ARI-809 normalizes elevated sorbitol and fructose levels in sciatic nerve tissues of diabetic rat models, inhibits sorbitol accumulation in lens tissues, and brings elevated urinary albumin excretion close to normal. ARI-809 can be used in diabetes research.
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- No. CAS: 463976-07-0
- Fòrmula: C13H9ClN2O4S
- Peso molecular:324.74
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
ARI-809 (CP-744809) shows high selectivity for aldose reductase over related dehydrogenases, with the lowest off-target potency against aldehyde reductase (IC50 = 930 nM) and minimal activity against alcohol, fructose, and sorbitol dehydrogenases[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Bioavailability | Cmax | T1/2 |
|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | p.o. | 98 % | 5 μg/mL | 26 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD Sprague Dawley (male, 175-225 g, streptozotocin-induced)[1]
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Dosage:0.2 mg/kg (acute sciatic nerve sorbitol normalization); 0.8 mg/kg (acute sciatic nerve fructose normalization; chronic sciatic nerve sorbitol normalization); 4.0 mg/kg (chronic sciatic nerve fructose normalization)
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Administration:oral gavage; single doses at 4,7,24h post-streptozotocin (acute); once daily for 5 days (chronic)
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Result:Achieved an ED50 of 0.2 mg/kg for normalization of elevated sciatic nerve sorbitol levels in acute test.
Achieved an ED50 of 0.8 mg/kg for normalization of elevated sciatic nerve fructose levels in acute test.
Achieved an ED90 of 0.8 mg/kg for normalization of elevated sciatic nerve sorbitol levels in chronic test.
Achieved an ED90 of 4.0 mg/kg for normalization of elevated sciatic nerve fructose levels in chronic test.
Potently suppressed elevated lens sorbitol levels, with greater efficacy than comparator agents including zopolrestat.
Produced near-normalization of 2.5-fold elevated urinary albumin output in a diabetic rat model.
Chemical Information
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No. CAS 463976-07-0
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Peso molecular 324.74
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Fòrmula C13H9ClN2O4S
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SMILES
O=C1C=CC(S(=O)(C2=C(C)C3=CC(Cl)=CC=C3O2)=O)=NN1
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Synonyms
CP-744809
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ARI-809 Related Classifications
HY-119058 Related Classifications
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