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Cyclosporin A


CAS No. : 59865-13-3

(Synonyms: Cyclosporine A; Ciclosporin A; CsA)

59865-13-3
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Cat. No. : HY-B0579
M.Wt: 1202.61
Formula: C62H111N11O12
Purity: >98 %
Solubility: DMSO : 62.5 mg/mL (ultrasonic);Ethanol : 50 mg/mL (ultrasonic)
Introduction of 59865-13-3 :

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]. 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: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].

Pharmacokinetic parameters of blood showed area under the curve of 27.3 μg·h·mL-1, half-life of 6.9 h, volune of distribution of 3.7 L/kg in 140-200 g, 5-6 weeks, twelve adult male Wistar rats (Cyclosporin A 10 mg/kg; iv)[9].Blood pharmacokinetic parameters shows: Cyclosporin A (10 mg/kg; iv) has an area of the curve of 27.3 μg·h·mL-1 and a half-life of 6.9 h, and the distribution volume of 3.7 L/kg in male Wistar rats (140-200 g, 5-6 weeks)[9].
1. Induction of Uraemia[10][11]
Background
Cyclosporin A administration induces interstitial deposition of collagen type III and fibrosis via stimulation of the Transforming Growth Factor beta (TGF-β)-signalling pathway, while inhibiting extracellular matrix (ECM) degradation via modulation of matrix metallopeptidase 9, thus leading to an imbalance in ECM turn over[2].
Specific Mmodeling Methods
Mice: Six-to-eight weeks old C57BL/6 mice
Administration: 30 mg/kg • SC • daily for 16 weeks.
Modeling Indicators
Molecular changes: Upregulated mRNA expression of both LOX, LOXL2, TNFα, MCP-1, (NOX)4; significantly downregulated SOD2 mRNA expression; increased the urea nitrogen (BUN) level, increased tubular injury, interstitial inflammation and fibrosis scores, PAS scores, increased the level the deposition of collagen type I (COL1) and type III (COL3) in the renal ECM,increased the expression of alpha-smooth-muscle actin (α-SMA), fibronectin (FN), COL1A, MCP-1[10][11].
Correlated Product(s):
Opposite Product(s):Lipoxygenase, general (HY-P2976); Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11) (HY-P990107)

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