Deflazacort Glucocorticoid Receptor agonist

Deflazacort (MDL 458) is a glucocorticoid used as an anti-inflammatory and immunosuppressant.

Deflazacort  Glucocorticoid Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 441.52

Purity & Quality Control

Batch: S188801 DMSO]88 mg/mL]false]Ethanol]12 mg/mL]false]Water]Insoluble]false Purity: 99.91%
99.91

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Mechanism of Action

Targets
Glucocorticoid receptor [1]

In Vivo

In vivo Deflazacort results in a significant and equal decrease of thymus weight, indicating a marked reduction in total immunogenic tissue in rats. [1] This compound reduces thymus weight and Daily weight gain in rats. It lowers liver IFG-I and GHR mRNA in rats. [2] This chemical is a heterocyclic glucocorticoid with anti-inflammatory activity but with decreased side effects. It and [3H]dexamethasone (DEX) similarly induce in vivo ornithine decarboxylase activity in hippocampus and liver, although body weight loss after chronic treatment is significantly less for DFC. [3] This compound induces dose-dependent decreases in osteocalcin (OC) plasma production rate (PPR). It and prednisolone increase both postabsorptive plasma glucose and plasma calcium levels in sheep, but there are no significant differences between their effects. [4] This compound, especially combined with L-arginine, spares quadriceps muscle from injury-induced regeneration (myf5 expression) compared with placebo treatment, despite an increase in membrane permeability immediately after exercise. It alone prevents the typical progressive loss of function (measured as voluntary distance run over 24 hours) that is observed 3 months later in placebo-treated mice. [5] It causes a less significant alteration in the pattern of GH secretion and does not negatively affect the overall amount of GH secreted. [6]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04791345 Unknown status
Healthy Volunteers
Parc de Salut Mar
February 26 2021 Phase 1
NCT03783923 Terminated
Limb-Girdle Muscular Dystrophy
PTC Therapeutics
October 31 2019 Phase 3
NCT03642145 Withdrawn
Duchenne Muscular Dystrophy
PTC Therapeutics
October 31 2018 Phase 3
NCT02251600 Completed
Duchenne Muscular Dystrophy
PTC Therapeutics
December 2014 Phase 1
NCT02286622 Completed
Renal Impairment
PTC Therapeutics
December 2014 Phase 1

References

  • https://pubmed.ncbi.nlm.nih.gov/22192593/
  • https://pubmed.ncbi.nlm.nih.gov/7804450/
  • https://pubmed.ncbi.nlm.nih.gov/8003438/
  • https://pubmed.ncbi.nlm.nih.gov/8402319/
  • https://pubmed.ncbi.nlm.nih.gov/16464957/
  • https://pubmed.ncbi.nlm.nih.gov/10229911/

Chemical Information

Molecular Weight 441.52 Formula

C25H31NO6

CAS No. 14484-47-0 SDF Download SDF
Synonyms MDL 458
Smiles CC1=NC2(C(O1)CC3C2(CC(C4C3CCC5=CC(=O)C=CC45C)O)C)C(=O)COC(=O)C

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (199.31 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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