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Methylprednisolone Glucocorticoid Receptor agonist

Cat.No.S1733

Methylprednisolone is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. This compound activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. It markedly reduces autophagy and apoptosis.
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Quality Control

Batch: Purity: 99.96%
99.96

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 cells Function assay 24 h Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis, EC50=4 μM
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Solubility

In vitro
Batch:

DMSO : 75 mg/mL (200.28 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

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In vivo
Batch:

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 374.47 Formula

C22H30O5

Storage (From the date of receipt)
CAS No. 83-43-2 Download SDF Storage of Stock Solutions

Synonyms NSC-19987, U 7532 SMILES CC1CC2C3CCC(C3(CC(C2C4(C1=CC(=O)C=C4)C)O)C)(C(=O)CO)O

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Mechanism of Action

Targets/IC50/Ki
Glucocorticoid receptor
In vitro

Methylprednisolone (2-10 mg/kg) markedly inhibits TNF production but does not affect serum levels of IL-10, while a high dose of this compound (50 mg/kg) increases LPS-induced IL-10 levels. This chemical (from 0.01 to 100 mg/mL) also increases the biosynthesis of IL-10 by LPS-activated mouse peritoneal macrophages.

In vivo

Methylprednisolone decreases RGC survival in rats with electrophysiologically diagnosed optic neuritis. This compound decreases RGC survival by a nongenomic, calcium-dependent mechanism. Its induced enhancement of RGC degeneration depends on calcium influx through voltage-gated calcium channels. This treatment leads to a significant decrease in the number of ED1-positive cells in both rostral and caudal stumps. It results in a significant reduction in tissue loss in both cord stumps at 2, 4 and 8 week post-injury. This chemical leads to a long-term reduction of ED1-positive cells and spinal tissue loss, reduced dieback of vestibulospinal fibres, and a transient sprouting of vestibulospinal fibres near the lesion at 1 and 2 weeks post-lesion. At a dose of 30 mg/kg which has been shown to be effective in improving functional outcomes in rat SCI models, it suppresses TNF-α expression and NF-kB activation. Its inhibition of NF-kB function is likely mediated by the induction of IkB, which traps NF-kB in inactive cytoplasmic complexes.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/9729336/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-30)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07072585 NOT_YET_RECRUITING
Stage II T Lymphoblastic Leukemia/Lymphoma; Stage III T Lymphoblastic Leukemia/Lymphoma; Stage IV T Lymphoblastic Leukemia/Lymphoma; T Acute Lymphoblastic Leukemia; T Lymphoblastic Lymphoma
Children's Oncology Group
2026-08-28 PHASE2; PHASE3
NCT07478003 RECRUITING
STEMI - ST Elevation Myocardial Infarction
Thomas Engstrom
2026-04-20 PHASE3
NCT07258771 RECRUITING
Ulcerative Colitis Acute
Berinstein, Jeffrey
2026-01-16 PHASE4
NCT06970743 ACTIVE_NOT_RECRUITING
Chronic Lymphocytic Leukemia; Small Lymphocytic Lymphoma
BeOne Medicines
2025-05-29 PHASE3
NCT07703098 NOT_YET_RECRUITING
Adrenal Insufficiency
University Medical Centre Ljubljana
2026-09-01 PHASE4
NCT07412470 RECRUITING
Kidney Transplant Rejection
Sanofi
2026-03-13 PHASE2; PHASE3

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