Cyclosporin A
- 貨號 Cat. No.
- C-900
- 規格 Size
- 25 mg 5x25mg 100mg
Description
Cyclosporin A
| Product#: | C-900 |
| Sizes: |
| 25 mg |
| 5 x 25 mg |
| 100 mg |
| M.W.: | 1202.61 |
| Structure: |
. |
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| Purity: | >97% |
| Bioassay: |
| The biological activity of Cyclosporin A was tested to demonstrate its ability to inhibit the anti-adipogenic effect of Ca2+ -dependent protein phosphatases (calcineurin). |
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| 3T3-L1 preadipocytes were induced to undergo differentiation with 1 mg/ml insulin for 4 days (A,B and C). The cells were treated for the first 4 days of differentiation with 1mM Ionomycin (B-D) in the presence of 10 ng/ml (C) or 50 ng/ml (D) Cyclosporin A. After 10 days, the cells were stained with Oil Red O and visualized with light microscopy. |
| References: |
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2. | Breuder, T. et al. (1994) Proc. Natl. Acad. Sci. U. S. A. 91, 5372. |
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4. | Cardenas, M. E. et al. (1998) Trends Biotechnol. 16, 427. |
5. | Guerini, D. (1997) Biochem. Biophys. Res. Commun. 235, 271. |
6. | Schreiber, S.L. and Crabtree, G.R. (1992) Immunol.Today 13, 136. |
7. | Graef, I.A. et al. (2001) Cell 105, 863. |
8. | Cyert, M. S. et al. (1991) Proc. Natl. Acad. Sci. U. S. A. 88, 7376. |
9. | Ye, R.R. and Bretscher, A. (1992) Eur. J. Biochem. 204, 713. |
10. | Cyert, M. S. and Thorner, J. (1992) Mol. Cell. Biol. 12, 3460. |
11. | Horsley, V. and Pavlath, G.K. (2002) J.Cell Biol. 156, 771. |
12. | Flanagan, W.M. et al. (1991) Nature 352, 803. |
13. | Clipstone, N.A. and Crabtree, G.R. (1992) Nature 357, 695. |
14. | O'Keefe, S.J. et al. (1992) Nature 357, 692. |
15. | Ruqin, K. et al. (2002) J. Biol. Chem. 277, 29669. |
16. | Andres, D. et al. (2001) Biochem. Pharmacol. 61, 427. |
17. | Perry, S.S. et al. (1999) Cell Transplant. 8, 339. |
18. | Tavares, P. et al. (1998) J. Cardiovasc. Pharmacol. 31, 46. |
19. | Twentyman, P.R. et al. (1992) Br. J. Cancer. 65, 335. |
20. | Esposito, C. et al. (2000) Kidney Int. 58, 123. |
21. | Nickoloff, B.J. et al. (1988) Am. J. Pathol. 131, 12. |
22. | Bell, A. et al. (1994) Biochem Pharmacol. 48, 495. |
Cyclosporin A is a hydrophobic cyclic peptide isolated from Tolypocladium inflatum and is a potent immunosuppressant and antifungal compound. It acts via its ability to binds a family of intracellular proteins, the cyclophilins (intracellular peptidyl-prolyl cis-trans isomerases), which are abundant, ubiquitous, highly conserved, and found in multiple forms in different intracellular compartments.1 In yeast, Cyclophilin A, an 18-kDa cytoplasmic protein, mediates Cyclosporin A actions.2, 3
The immunosuppressive action of Cyclosporin A is mediated by the complex Cyclosporin A-Cyclophilin that specifically inhibits the Ca2+/calmodulin-dependent serine-threonine-protein phosphatase-2B (Calcineurin).4-10 This in turn inhiibts the Calcineurin and promotes dephosphorylation of transcription factor NF-AT and T-cell activation.11-14 In vivo, Cyclosporin A - induced hypertension involves, the attenuation of endothelium-derived NO production through inhibition of Calcineurin-sensitive pathway regulating eNOS dephosphorylation.15
Cyclosporin A has been shown to alter cell proliferation in different systems. For hematopoietic progenitor stem and progenitor cells, smooth muscle cells, and hepatocytes, it serves as an inducer of cell proliferation or a tumor promoting effector.16-18 On the other hand, growth of interleukin-3-dependent mast cells, human lung-cancer cells, tubular kidney cells, cultured pituitary cells, T-cells, and keratinocytes were inhibited by Cyclosporin A.19-21 Moreover, Cyclosporin A has been observed in vitro and in vivo as an antimalarial agent, but the exact mechanism is not yet clear.22

