Cyclosporin A  (Synonyms: Cyclosporine A; Ciclosporin A; CsA)

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 also inhibits CD11a/CD18 adhesion^[8].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1202.61

C₆₂H₁₁₁N₁₁O₁₂

59865-13-3

Solid

White to off-white

C/C=C/C[C@H]([C@@H](O)[C@@]1(N(C)C([C@]([H])(C(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@]([H])(CC(C)C)N(C)C([C@@H](C)NC([C@H](C)NC([C@@H](N(C([C@@]([H])(NC([C@@H](N(C(CN(C([C@@H](NC1=O)CC)=O)C)=O)C)CC(C)C)=O)C(C)C)=O)C)CC(C)C)=O)=O)=O)=O)=O)=O)[H])C

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Handschumacher RE, et al. Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science. 1984 Nov 2;226(4674):544-7.  [Content Brief]

  [2]. Liu J, et al. Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell. 1991 Aug 23;66(4):807-15.  [Content Brief]

  [3]. Fruman DA, et al. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A. Proc Natl Acad Sci U S A. 1992 May 1;89(9):3686-90.  [Content Brief]

  [4]. Flanagan WM, et al. Nuclear association of a T-cell transcription factor blocked by FK-506 and cyclosporin A. Nature. 1991 Aug 29;352(6338):803-7.  [Content Brief]

  [5]. Nicolli A, et al. Interactions of cyclophilin with the mitochondrial inner membrane and regulation of the permeability transition pore, and cyclosporin A-sensitive channel. J Biol Chem. 1996 Jan 26;271(4):2185-92.  [Content Brief]

  [6]. Borel JF, et al. Effects of the new anti-lymphocytic peptide cyclosporin A in animals. Immunology. 1977 Jun;32(6):1017-25.  [Content Brief]

  [7]. Williams, R, et al. Randomised trial comparing FK506 and cyclosporin in prevention of liver allograft rejection. European FK506 Multicentre Liver Study Group. Lancet, 1994, 344(8920), 423-428.  [Content Brief]

  [8]. Dalmarco EM, et al. Cyclosporin A inhibits CD11a/CD18 adhesion molecules due to inhibition of TNFalpha and IL-1 beta levels in the mouse model of pleurisy induced by carrageenan. Cell Adh Migr. 2008 Oct-Dec;2(4):231-5.  [Content Brief]

  [9]. Medeiros M, et al. Increased cyclosporine bioavailability induced by experimental nephrotic syndrome in rats. Can J Physiol Pharmacol. 2007 May;85(5):502-6.  [Content Brief]

  [10]. Nguyen LT, et al. Lysyl oxidase inhibitors attenuate cyclosporin A-induced nephropathy in mouse. Sci Rep. 2021 Jun 14;11(1):12437.  [Content Brief]

  [11]. Ling H, et al. Therapeutic role of TGF-beta-neutralizing antibody in mouse cyclosporin A nephropathy: morphologic improvement associated with functional preservation. J Am Soc Nephrol. 2003 Feb;14(2):377-88.  [Content Brief]