Cyclosporine

SKU: orb1310145

Description

Cyclosporin A

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 59865-13-3
• MW: 1202.7
• Purity: >99%
• Formula: C₆₂H₁₁₁N₁₁O₁₂
• SMILES: [C@H]([C@@H](C/C=C/C)C)(O)[C@@]1(N(C)C(=O)[C@H]([C@@H](C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H]([C@H](C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C(=O)[C@H](CC)NC1=O)[H]
• Target: Phosphatase
• Solubility: Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 25 mg/ml).

Bioactivity

• Target IC50:
  U-87MG cells viability:10 μM|CYP450 (Rat):0.4 μM (Ks)|Calcineurin phosphatase:7 nM
• In Vivo:
  METHODS: To assay activity against muscle disease in vivo, Cyclosporin A (5 mg/kg in olive oil) was injected intraperitoneally into myopathic Col6a1-/- mice twice daily for ten days. RESULTS: Cyclosporin A affected satellite cell activity and triggered regenerative fiber formation in Col6a1-/- mice. METHODS: To detect the effects on ischemia-reperfusion injury (IRI), Cyclosporin A (3 mg/kg, 1 h or 10 min before ischemia; 10 mg/kg, 10 min before ischemia) was intraperitoneally injected into ischemia-reperfused C57BL/6J mice. RESULTS: Mortality and renal function were significantly higher in the Cyclosporin A 10 mg/kg-10 min and Cyclosporin A 3 mg/kg-1 h groups than in the Cyclosporin A 3 mg/kg-10 min group.
• In Vitro:
  METHODS: Glioma cell C6 was treated with Cyclosporin A (10 μM) under hypoxic conditions for 4 h. The expression levels of target proteins were measured by Western Blot. RESULTS: 4 h hypoxia induced a large accumulation of endogenous HIF-1α protein, and Cyclosporin A prevented most of the hypoxia-induced HIF-1α stabilization. METHODS: Human colon cancer cells CACO-2 were treated with Cyclosporin A (2 μM) for 24-72 h. The cell cycle was detected by Flow Cytometry. RESULTS: Accumulation of cells was detected in the G0/G1 phase after treatment with Cyclosporin A. The RESULTS were summarized in the following table.
• Cell Research:
  Immunosuppressive agents are dissolved in ethanol at concentrations 1000-fold more than the concentration desired for cell treatments. Cells (106) are suspended in 1 ml of complete medium in microcentrifuge tubes; 1 μl of ethanol or of the ethanolic solution of Cyclosporin A is added, and the cells are incubated at 37°C for 1 hr. Cells are washed twice with 1 ml of PBS on ice and lysed in 50μl of hypotonic buffer containing 50 mM Tris (pH 7.5); 0.1 mM EGTA; 1 mM EDTA; 0.5 mM dithiothreitol; and 50 μg of phenylmethylsulfonyl fluoride, 50 μg of soybean trypsin inhibitor, 5 μg of leupeptin, and 5 μg of aprotinin per ml. Lysates are subjected to three cycles of freezing in liquid nitrogen followed by thawing at 30°C and then are centrifuged at 4°C for 10 min at 12,000×g.(Only for Reference)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cyclosporin A

Compound Identifiers

PubChem CID

5284373