Methylprednisolone succinate

Methylprednisolone succinate (Methylprednisolone hydrogen succinate) is a prodrug of Methylprednisolone (HY-B0260) and glucocorticoid with immunosuppressant and anti-inflammatory activity. Methylprednisolone succinate binds cytosolic glucocorticoid receptors, translocates to nuclei, and modulates target gene transcription. Methylprednisolone succinate alters Bax, Bcl-2, occludin, and ZO-1 expression; attenuates TLR4/NF-κB signaling; suppresses proinflammatory cytokine production and immune cell activation. Methylprednisolone succinate can be used for the research of intracranial haemorrhage, rheumatoid arthritis, multiple sclerosis, preterminal cancer, inflammatory conditions, shock, immediate-type hypersensitivity, acute myocardial ischemia, hypoxic heart muscle damage, and traumatic spinal cord injury^{[1][2][3][4][5][6]}. IC50 & Target:glucocorticoid receptor^[1] In Vitro:Methylprednisolone succinate (0.4-1.25 mg/mL methylprednisolone equivalent; 24 h at 24°C) is chemically stable and visually compatible in admixtures with Cimetidine hydrochloride (HY-14289A) (3 mg/mL) in 5% dextrose injection, with no significant loss of methylprednisolone 21-succinate ester concentration^[2]. In Vivo:Methylprednisolone succinate (30 mg/kg; i.p.; at 2, 24, and 48 h after ICH) suppresses inflammatory responses, attenuates BBB disruption, and reduces neuronal apoptosis in a mouse model of intracranial haemorrhage^[1].
Methylprednisolone succinate (40 mg/kg; slow administration over 1 minute) improves collateral blood flow into the infarcted area and enhances the metabolic response of ischemic myocardium in acute myocardial ischemia dogs^[5].