Cyclosporin A-d₁₂  (Synonyms: Cyclosporine A-d₁₂; Ciclosporin A-d₁₂; CsA-d₁₂)

Cyclosporin A-d₁₂ (Cyclosporine A-d₁₂) is deuterium labeled 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 also inhibits CD11a/CD18 adhesion^[8].

氢、碳和其他元素的稳定重同位素已被掺入药物分子中，主要用作药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注。

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

1214.69

C₆₂H₉₉D₁₂N₁₁O₁₂

59865-13-3

环胞霉素A-d₁₂

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. 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]

  [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]. 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]

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

  [10]. 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]

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

  [12]. 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]