M 16287
M 16287 is an orally active aldose reductase inhibitor, with an IC50 of 0.08 μM in rats and 0.25 μM in cattle. M 16287 improves lens fiber swelling and vacuolization, prevents galactitol accumulation, delays inositol depletion, inhibits glutathione reduction, restores the NADPH/NADP+ ratio to normal, and normalizes lens Na+ content and Na+/K+ ratio. M 16287 prevents galactose-induced cataract formation in rats. M 16287 improves motor nerve conduction velocity in diabetic rats, partially alleviates histopathological changes in the sciatic nerve, and inhibits sorbitol accumulation. M 16287 can be used in studies related to cataracts and diabetic neuropathy.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 128851-55-8
- 分子式: C11H7ClN2O5S
- 分子量:314.70
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
M16287 potently inhibits partially purified rat lens aldose reductase with an IC50 of 0.08 μM and partially purified bovine lens aldose reductase with an IC50 of 0.25 μM[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
M16287 (3-100 mg/kg; p.o.; once daily; for 14 consecutive days) dose-dependently improves motor nerve conduction velocity, inhibits sorbitol accumulation, and partially ameliorates histological changes in the sciatic nerve of Streptozotocin (HY-13753)-induced diabetic rats. When treatment is initiated earlier at 4 days after diabetes induction, it exerts a more significant inhibitory effect on sorbitol accumulation in the sciatic nerve and lens of streptozotocin-induced diabetic rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 90-120 g, galactose-induced cataract model)[1]
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Dosage:10 mg/kg/day; 30 mg/kg/day; 100 mg/kg/day
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Administration:p.o.; daily; up to 15 days
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Result:Inhibited galactose-induced cataract progression dose-dependently, fully blocking lesions at 100 mg/kg/day and nearly suppressing formation at 30 mg/kg/day, while alleviating lens swelling, liquefaction and vacuolation.
Dose-dependently lowered lens galactitol, slowed myo-inositol depletion and restrained glutathione loss across all observation time points.
Regulated lens NADPH/NADP+ pools and decreased sodium content as well as Na+/K+ ratio on day 15 without obvious recovery of potassium levels.
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Animal Model:Wistar (male, 150-180 g, Streptozotocin-induced diabetic neuropathy, treatment initiated 14 days post-induction)[2]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Elevated sciatic motor nerve conduction velocity dose-dependently with significant effects at 30 and 100 mg/kg.
Dose-dependently lowered sorbitol build up in sciatic nerve and lens, with marked suppression at 30 and 100 mg/kg.
Failed to alter sciatic nerve myo-inositol content and only partially rescued lens myo-inositol loss at high doses.
Shifted sciatic nerve myelinated fiber distribution at 30 mg/kg by reducing thin fibers and expanding medium-sized fiber proportion.
Exerted no influence on body weight or serum glucose concentrations.
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Animal Model:Wistar (male, 150-180 g, Streptozotocin-induced diabetic neuropathy, treatment initiated 4 days post-induction)[2]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Exhibited stronger dose-dependent suppression of sorbitol buildup in sciatic nerve and lens, with significant declines at 30 and 100 mg/kg.
Failed to modify sciatic nerve myo-inositol levels.
Only partially reversed lens myo-inositol depletion at high doses.
化学情報
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CAS 番号 128851-55-8
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分子量 314.70
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分子式 C11H7ClN2O5S
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SMILES
O=C1NC(=O)CN1S(=O)(=O)C=2OC=3C=CC=CC3C2Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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
参考文献
[1]. Kato K, et al. Effects of novel hydantoin derivatives with aldose reductase inhibiting activity on galactose-induced cataract in rats. Japanese journal of pharmacology. 1990 Dec;54(4):355-64. [Content Brief]
[2]. Kato K, et al. Effects of novel aldose reductase inhibitors, M16209 and M16287, on streptozotocin-induced diabetic neuropathy in rats. European journal of pharmacology. 1991 Feb 07;193(2):185-91. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
M 16287 関連分類
HY-165518 関連分類
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