Cyclosporin A

Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM^[3]. Cyclosporin A is a molecular glue, binds to cyclophilin and calcineurin, leading to inactivation of nuclear Factor of activated T Cells (NFAT) and a subsequent decrease in the immune response. Cyclosporin A also inhibits CD11a/CD18 adhesion^[8][9]. IC50 & Target:IC50: 7 nM (calcineurin) In Vitro:Cyclosporin A is able to bind with the cyclophilin in T cells^[1].
Cyclosporin A works by forming a Cyclophilin-Cyclosporin A complex to inhibit calcineurin^[2].
Cyclosporin A inhibits calcineurin in stimulated cells with an IC₅₀ value of 7 nM^[3].
Cyclosporin A suppresses the nuclear translocation of NF-AT^[4].
Cyclosporin A shows an effect on mitochondria via preventing the MTP from opening with an IC₅₀ of 39 nM^[5]. In Vivo:Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Cyclosporin A can be used to construct uremia models. In male Wistar rats (weighing 140-200 g, aged 5-6 weeks), the pharmacokinetic parameters following intravenous administration of Cyclosporin A (10 mg/kg) show an area under the curve of 27.3 μg·h/mL, a half-life of 6.9 hours, and a volume of distribution of 3.7 L/kg^[9].