Rimexolone

CAS No:
49697-38-3 Category:
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Product Details:

  • CAS No: 49697-38-3
  • AHFC code: 52:08.1
  • Synonyms:
  • ATC Code: H02AB12 S01BA13
  • Chemical Formula: C14H22N2O2
  • Molecular Weight: 370.525
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB00896 (APRD01220)
  • SMILES: CCC(=O)[C,,]1(C)[C,H](C)CC2C3CCC4=CC(=O)C=C[C,]4(C)C3[C,,H](O)C[C,]12C
  • InChl: QTTRZHGPGKRAFB-PAIWTFDUSA-N
  • PubChem: 5311412
  • IUPAC: (2R,13R,14S,15S,17S)-17-hydroxy-2,13,14,15-tetramethyl-14-propanoyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one

Additional Details

Indication:
For the treatment of postoperative inflammation following ocular surgery and in the treatment of anterior uveitis.
Pharmacodynamics:
Rimexolone is a glucocorticoid corticosteroid for systemic use. Corticosteroids suppress the inflammatory response to a variety of inciting agents of a mechanical, chemical, or immunological nature. They inhibit edema, cellular infiltration, capillary dilatation, fibroblastic proliferation, deposition of collagen and scar formation associated with inflammation.
Mode of Action:
Rimexolone is a glucocorticoid receptor agonist. The antiinflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition of arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. By binding to the glucocorticoid receptor, this drug ultimately leads to changes in genetic transcription involving the lipocortins and prostaglandins.
Metabolism:
Undergoes extensive metabolism. Following intravenous administration of radiolabeled rimexolone in rats, more than 80% of the dose was excreted in the feces as rimexolone and metabolites. Metabolites have been shown to be either less active than rimexolone or inactive in human glucocorticoid receptor binding assays.
Toxicity:
Symptoms of overdose include retinal toxicity, glaucoma, and subcapsular cataract.
General Reference:
Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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