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.
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- CAS. Nr.: 128851-55-8
- Formel: C11H7ClN2O5S
- Molecular Weight:314.70
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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.
Chemical Information
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CAS. Nr. 128851-55-8
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Molecular Weight 314.70
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Formel C11H7ClN2O5S
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SMILES
O=C1NC(=O)CN1S(=O)(=O)C=2OC=3C=CC=CC3C2Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
M 16287 Related Classifications
HY-165518 Related Classifications
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