2. Metabolic Enzyme/Protease
  3. Aldose Reductase
  4. 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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ARI-809

ARI-809 Chemical Structure

CAS No. : 463976-07-0

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ARI-809 Related Antibodies

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Description

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[1].

In Vitro

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.

ARI-809 Related Antibodies
Parmacokinetics
Species Dose Route Bioavailability Cmax T1/2
Rat[1] 2 mg/kg p.o. 98 % 5 μg/mL 26 h
In Vivo

ARI-809 (0.2-4.0 mg/kg; oral gavage; single doses at 4,7,24h post-streptozotocin '; once daily for 5 days (chronic)) potently normalizes elevated polyol pathway metabolites in diabetic rat sciatic nerve and lens tissues, with ED50 values of 0.2 mg/kg and 0.8 mg/kg for sorbitol and fructose normalization in the acute test, and ED90 values of 0.8 mg/kg and 4.0 mg/kg for sorbitol and fructose normalization in the chronic test, while also reducing urinary albumin output in diabetic rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD Sprague Dawley (male, 175-225 g, streptozotocin-induced)[1]
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)
Administration: oral gavage; single doses at 4,7,24h post-streptozotocin (acute); once daily for 5 days (chronic)
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.
Molecular Weight

324.74

Formula

C13H9ClN2O4S
CAS No.
SMILES

O=C1C=CC(S(=O)(C2=C(C)C3=CC(Cl)=CC=C3O2)=O)=NN1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ARI-809 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ARI-809463976-07-0CP-744809ARI809ARI 809CP744809CP 744809Aldose Reductasealdose reductasediabetic rat modelsaldehyde reductaseCaco-2lens tissuediabetes mellitusP450 enzymesciatic nerve tissueratspolyol pathwayInhibitorinhibitorinhibit

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