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

ARI-809 (CP-744809) 是一种高选择性的、口服有效的醛糖还原酶 (aldose reductase) 抑制剂，其 IC50 为 1 nM。ARI-809 可阻断多元醇通路中过量的葡萄糖流量。ARI-809 可使糖尿病大鼠模型坐骨神经组织中升高的山梨醇和果糖水平恢复正常，抑制晶状体组织中山梨醇的蓄积，并使升高的尿白蛋白排出量接近正常。ARI-809 可用于糖尿病的研究。

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ARI-809

ARI-809 Chemical Structure

CAS No. : 463976-07-0

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ARI-809 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

ARI-809 相对于相关脱氢酶表现出对醛糖还原酶的高选择性，其中对醛还原酶的脱靶活性最低 (IC50 = 930 nM)，且对乙醇脱氢酶、果糖脱氢酶和山梨醇脱氢酶的活性极低[1]。

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

ARI-809 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Bioavailability Cmax T1/2
Rat[1] 2 mg/kg p.o. 98 % 5 μg/mL 26 h
体内研究
(In Vivo)

ARI-809 (0.2-4.0 mg/kg；灌胃；单次给药 ；或每日 1 次，连续 5 天) 可强效逆转糖尿病大鼠坐骨神经和晶状体组织中升高的多元醇通路代谢物水平：在急性试验中，其使山梨醇和果糖水平恢复正常的 ED50 分别为 0.2 mg/kg 和 0.8 mg/kg；在慢性试验中，使山梨醇和果糖水平恢复正常的 ED90 分别为 0.8 mg/kg 和 4.0 mg/kg，同时还可降低糖尿病大鼠的尿白蛋白排泄量[1]。

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.
分子量

324.74

Formula

C13H9ClN2O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ARI-809 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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