Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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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. 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.
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].
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ln Vivo |
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Animal Protocol |
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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.
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Molecular Formula |
C25H31NO6
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Molecular Weight |
441.52
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CAS # |
14484-47-0
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Related CAS # |
Deflazacort-d5;Deflazacort-d7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC(OCC(C12N=C(C)OC1CC3C(CCC4=CC(C=C[C@@]45C)=O)C5[C@@H](O)C[C@@]32C)=O)=O
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Synonyms |
MDL 458; Cortax; Decortil; Deflanil; Flezacor; ML-458; ML458; DL-458-IT, L-5458; trade name: Emflaza
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.
Calculation results
Working concentration: mg/mL;
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.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.