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Art. -Nr.: HY-119058

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ARI-809

(Synonyms: CP-744809)

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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CAS. Nr.: 463976-07-0
Formel: C₁₃H₉ClN₂O₄S
Molecular Weight:324.74

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

ARI-809 Chemical Structure

CAS. Nr.: 463976-07-0

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

Parmacokinetics

Species	Dose	Route	Bioavailability	C_max	T_1/2
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.

Chemical Information

CAS. Nr. 463976-07-0
Molecular Weight 324.74
Formel C₁₃H₉ClN₂O₄S
SMILES

O=C1C=CC(S(=O)(C2=C(C)C3=CC(Cl)=CC=C3O2)=O)=NN1
Synonyms

CP-744809
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Mylari BL, et al. A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners. J Med Chem. 2005;48(20):6326-6339. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

100 mg

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