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Cyclosporine A

Cat. No. M1831
Cyclosporine A Structure
Synonym:

Cyclosporine

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 44  USD55 In stock
50mg USD 29.6  USD37 In stock
100mg USD 40  USD50 In stock
200mg USD 60  USD75 In stock
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Quality Control
Biological Activity

Cyclosporin A is an immunosuppressant that binds to cyclophilin and inhibits calcineurin with an IC50 of 7 nM. cyclosporin A [CsA] binds to the cyclophilin 18 (Cyp18)-CsA complex. the Cyp18-CsA complex recruits calcium-regulated neurophosphatase (CaN), leading to the blocking of cytokine gene transcription in activated T cells. CsA is a highly specific inhibitor of T-cell activation.

Customer Product Validations & Biological Datas
Source Can J Physiol Pharmacol (2014). Figure 2. Cyclosporine A
Method MTT assay
Cell Lines NRK-52E and LLC-PK1 cells
Concentrations 10 mg/L
Incubation Time 24 and 48 h
Results A noticeably higher susceptibility of the rat kidney cell line to toxicity in the presence of CyA in vehicle was noted compared with the pig kidney cell line
Source Can J Physiol Pharmacol (2014). Figure 1. Cyclosporine A
Method Hepatocytes
Cell Lines NL and HL rat
Concentrations 2.5 mg/L
Incubation Time 5 and 30 min
Results In the hepatocytes exposed to CyA–2% NL rat serum, there was an initial spike in the uptake of CyA by the cells regardless of pretreatment
Protocol
Cell Experiment
Cell lines Jurkat cells (clone J77)
Preparation method 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.
Concentrations ~100 nM
Incubation time 1 h
Animal Experiment
Animal models Rat
Formulation 0.5% solution of tragacanth
Dosages 45 mg/kg
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 1202.61
Formula C62H111N11O12
CAS Number 59865-13-3
Purity 100.00%
Solubility DMSO ≥ 45 mg/mL
Storage 2-8°C, dry, sealed, protect from light
References

[1] Goksu Erol et al. Drug Chem Toxicol. The protective effects of omega 3 fatty acids and sesame oil against cyclosporine A-induced nephrotoxicity.

[2] Borel JF, et al. Immunology. Effects of the new anti-lymphocytic peptide cyclosporin A in animals.

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Keywords: Cyclosporine A, Cyclosporine supplier, Immunology/Inflammation, inhibitors

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