Deflazacort (MDL 458)

Alias: MDL 458; Cortax; Decortil; Deflanil; Flezacor; ML-458; ML458; DL-458-IT, L-5458; trade name: Emflaza
Cat No.:V1709 Purity: ≥98%
Deflazacort (ML-458; ML458;DL-458-IT, L-5458;Cortax; Decortil; Deflanil; Flezacor;trade name:Emflaza)is a potent glucocorticoid drug approved for use as an anti-inflammatory and immunosuppressant.
Deflazacort (MDL 458) Chemical Structure CAS No.: 14484-47-0
Product category: Calcium Channel
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Deflazacort (ML-458; ML458; DL-458-IT, L-5458; Cortax; Decortil; Deflanil; Flezacor; trade name: Emflaza) is a potent glucocorticoid drug approved for use as an anti-inflammatory and immunosuppressant. It was approved by FDA in 2017 to treat patients age 5 years and older with Duchenne muscular dystrophy (DMD). Deflazacort is an inactive prodrug which is metabolized rapidly to the active drug 21-desacetyldeflazacort. Deflazacort results in a significant and equal decrease of thymus weight, indicating a marked reduction in total immunogenic tissue in rats. Deflazacort reduces thymus weight and Daily weight gain in rats. Deflazacort lowers liver IFG-I and GHR mRNA in rats.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
The inert prodrug deflazacort quickly transforms into the active metabolite 21-desacetyldeflazacort. After 1.3 hours, maximum 21-desacetyldeflazacort concentrations were measured, with an average of 116 ng/ml. The terminal half-life was 1.3 hours, and the average area under the curve was 280 ng/ml.h. Prednisolone and methylprednisolone were eliminated considerably slower than 21-desacetyldeflazacort[1].
ln Vivo
Deflazacort results in a significant and equal decrease of thymus weight, indicating a marked reduction in total immunogenic tissue in rats. Deflazacort reduces thymus weight and Daily weight gain in rats. Deflazacort lowers liver IFG-I and GHR mRNA in rats. Deflazacort (DFC) is a heterocyclic glucocorticoid with anti-inflammatory activity but with decreased side effects. Deflazacort 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. Deflazacort induces dose-dependent decreases in osteocalcin (OC) plasma production rate (PPR). Deflazacort and prednisolone increase both postabsorptive plasma glucose and plasma calcium levels in sheep, but there are no significant differences between their effects. Deflazacort, 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. Deflazacort 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. Deflazacort causes a less significant alteration in the pattern of GH secretion and does not negatively affect the overall amount of GH secreted.
Animal Protocol
N/A
Deflazacort results in a significant and equal decrease of thymus weight, indicating a marked reduction in total immunogenic tissue in rats. Deflazacort reduces thymus weight and Daily weight gain in rats. Deflazacort lowers liver IFG-I and GHR mRNA in rats.
References
[1]. Mollmann, H., et al., Pharmacokinetic/pharmacodynamic evaluation of deflazacort in comparison to methylprednisolone and prednisolone. Pharmaceutical research, 1995. 12(7): p. 1096-1100.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C25H31NO6
Molecular Weight
441.52
CAS #
14484-47-0
Related CAS #
Deflazacort-d5;Deflazacort-d7
SMILES
CC(OCC(C12N=C(C)OC1CC3C(CCC4=CC(C=C[C@@]45C)=O)C5[C@@H](O)C[C@@]32C)=O)=O
Synonyms
MDL 458; Cortax; Decortil; Deflanil; Flezacor; ML-458; ML458; DL-458-IT, L-5458; trade name: Emflaza
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:88 mg/mL (199.3 mM)
Water:<1 mg/mL
Ethanol:12 mg/mL (27.1 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2649 mL 11.3245 mL 22.6490 mL
5 mM 0.4530 mL 2.2649 mL 4.5298 mL
10 mM 0.2265 mL 1.1325 mL 2.2649 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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