Methylprednisolone

Synonyms: NSC-19987, U 7532

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

Methylprednisolone Chemical Structure

Methylprednisolone Chemical Structure

CAS No. 83-43-2

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Cell Data

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 20966043
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Biological Activity

Description Methylprednisolone is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
Targets
Glucocorticoid receptor [1]
In vitro
In vitro

Methylprednisolone (2-10 mg/kg) markedly inhibits TNF production but does not affect serum levels of IL-10, while a high methylprednisolone dose (50 mg/kg) increases LPS-induced IL-10 levels. Methylprednisolone(from 0.01 to 100 mg/mL) also increases the biosynthesis of IL-10 by LPS-activated mouse peritoneal macrophages. [1]

In Vivo
In vivo

Methylprednisolone decreases RGC survival in rats with electrophysiologically diagnosed optic neuritis. Methylprednisolone decreases RGC survival by a nongenomic, calcium-dependent mechanism. Methylprednisolone-induced enhancement of RGC degeneration depends on calcium influx through voltage-gated calcium channels. [2] Methylprednisolone treatment leads to a significant decrease in the number of ED1-positive cells in both rostral and caudal stumps. Methylprednisolone treatment results in a significant reduction in tissue loss in both cord stumps at 2, 4 and 8 week post-injury. Methylprednisolone 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. [3] Methylprednisolone at a dose of 30 mg/kg which has been shown to be effective in improving functional outcomes in rat SCI models, suppresses TNF-α expression and NF-kB activation. Methylprednisolone inhibition of NF-kB function is likely mediated by the induction of IkB, which traps NF-kB in inactive cytoplasmic complexes. [4]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06343792 Not yet recruiting
Steroid Refractory GVHD
ReAlta Life Sciences Inc.
May 2024 Phase 2
NCT06297486 Recruiting
Hemophilia A
Spark Therapeutics Inc.
March 13 2024 Phase 3
NCT04560582 Withdrawn
Kidney Transplant; Complications|Kidney Transplant Rejection|Kidney Transplant Failure
University of Minnesota
September 22 2022 --
NCT04796493 Active not recruiting
Mesenteric Traction Syndrome
Rigshospitalet Denmark
March 16 2021 --
NCT04780581 Terminated
Corona Virus Infection
Fundación Instituto de Estudios de Ciencias de la Salud de Castilla y León|Instituto de Investigación Biomédica de Salamanca
February 1 2021 Phase 4

Chemical Information & Solubility

Molecular Weight 374.47 Formula

C22H30O5

CAS No. 83-43-2 SDF Download Methylprednisolone SDF
Smiles CC1CC2C3CCC(C3(CC(C2C4(C1=CC(=O)C=C4)C)O)C)(C(=O)CO)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 75 mg/mL ( (200.28 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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In vivo
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