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製品番号: HY-119058

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ARI-809

(別名: 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 番号: 463976-07-0
分子式: C₁₃H₉ClN₂O₄S
分子量:324.74

保管条件:

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

ARI-809 構造式

CAS 番号: 463976-07-0

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生物活性
- 製品説明
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
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生物活性

製品説明

体外実験

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

体内実験

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.

化学情報

CAS 番号 463976-07-0
分子量 324.74
分子式 C₁₃H₉ClN₂O₄S
SMILES

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

CP-744809
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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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