tcsc2761 Cyclosporin A

Cyclosporin A is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC₅₀ of 5 nM.

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 exhibits inhibitory effect on calcineurin with an IC₅₀ 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: Cyclosporin A has immunosuppressive activity, and is active via parenteral and p.o. administration in mice, rat and guinea pigs^[6]. Cyclosporin A can be used in organ transplantation to prevent rejection^[7].