Methylprednisolone Inhibitor CAS No. 83-43-2 - Methylprednisolone Supplier

Product Name	Methylprednisolone
Synonyms	Medrol, Meprolone
CAS No.	83-43-2
Molecular Weight	374.47
Formula	C₂₂H₃₀O₅
Chemical Name	6alpha-Methyl-1,4-pregnadiene-11beta,17alpha,21-triol-3,20-dione
Smiles	C1(=O)C=C[C@]2(C(=C1)[C@H](C[C@H]1[C@@H]3CC[C@](C(=O)CO)([C@@]3(C)C[C@@H]([C@H]21)O)O)C)C
Chemical Structure

Biological activities

Methylprednisolone is a synthetic glucocorticoid or corticosteroid drug. Methylprednisolone has anti-inflammatory effects. The IC50 value of methylprednisolone for suppression of T-helper cells is 4.6 ng/mL. The IC50 value of methylprednisolone for suppression of cortisol secretion is 0.8 ng/mL.^[1] The IC50s of methylprednisolone on rat blood and spleen lymphocytes in vitro are 1.38 and 3.1 nM, respectively.^[2] Methylprednisolone also can reduce the bulk flow of water across an in vitro blood-brain barrier.^[3] Methylprednisolone greatly inhibits the activity of calpain purified from rabbit muscle in a dose-dependent fashion.^[4] In a model system using the 16-h polyvinyl sponge implant in the rat in vivo, large intravascular doses of methylprednisolone (60 mg/kg) markedly inhibits neutrophil influx into sponges and adjacent connective tissue.^[5]

References

[1] Chow FS, et al. Modeling interactions between adrenal suppression and T-helper lymphocyte trafficking during multiple dosing of methylprednisolone. J Pharmacokinet Biopharm. 1999, 27(6): 559-575. [2] Rensberger KL, et al. Dextran-methylprednisolone succinate as a prodrug of methylprednisolone: in vitro immunosuppressive effects on rat blood and spleen lymphocytes. Int J Pharm. 2000, 207(1-2): 71-76. [3] Olson JJ, et al. Methylprednisolone reduces the bulk flow of water across an in vitro blood-brain barrier. Brain Res. 1988, 439(1-2): 259-265. [4] Banik NL, et al. A new mechanism of methylprednisolone and other corticosteroids action demonstrated in vitro: inhibition of a proteinase (calpain) prevents myelin and cytoskeletal protein degradation. Brain Res. 1997, 748(1-2): 205-210. [5] Wiener SL, et al. The mechanism of action of a single dose of methylprednisolone on acute inflammation in vivo. J Clin Invest. 1975, 56(3): 679-689.

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