Voclosporin, CAS 515814-01-4

Formulation: A solid

Formal Name: 6-[(2S,3R,4R,6E)-3-hydroxy-4-methyl-2-(methylamino)-6,8-nonadienoic acid]-cyclosporin A

Purity: ≥98%

Formula Markup: C63H111N11O12

Formula Weight: 1214,6

Shelf life (days): 1460

CAS Number: 515814-01-4

Notes: Voclosporin is an immunosuppressant and a derivative of cyclosporin A (Item No. 12088).{69624,69625} It binds to cyclophilin A (Kd = 15 nM) and inhibits calcineurin activity in isolated human whole blood (IC50 = 120 ng/ml). Voclosporin reduces the proliferation of, and production of IL-2, IFN-γ, and TNF-α in, isolated cynomolgus monkey lymphocytes (EC50s = 202.79, 135.32, 177.11, and 138.56 ng/ml, respectively).{69626} It decreases disease severity in a rat model of experimental autoimmune uveoretinitis induced by interphotoreceptor retinoid-binding protein (IRBP), also known as retinoid binding protein 3 (RBP3), when administered at doses ranging from 2.5 to 40 mg/kg.{69627} Voclosporin (1.75 mg/kg) increases graft survival in a rat model of heterotopic heart transplantation.{69625} Unlike cyclosporin A, voclosporin does not increase serum creatinine levels in rabbits. Voclosporin also inhibits the replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in infected Calu-3 cells in a concentration-dependent manner.{69628} Formulations containing voclosporin have been used in the treatment of lupus nephritis.

• Artikelnummer: CAY39719-5
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 39719-5
• Verpackungseinheit: 5 mg
• Mengeneinheit: STK