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.
Stem Cell Rev Rep. 2022 Jun 20.
Promoting Oligodendrocyte Differentiation from Human Induced Pluripotent Stem Cells by Activating Endocannabinoid Signaling for Treating Spinal Cord Injury
Cyclosporine A purchased from AbMole
J Ethnopharmacol. 2022 Sep 15;295:115409.
Senegenin alleviates Aβ1-42 induced cell damage through triggering mitophagy
Cyclosporine A purchased from AbMole
 |
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 |
| 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 |
| Molecular Weight | 1202.61 |
| Formula | C62H111N11O12 |
| CAS Number | 59865-13-3 |
| Solubility (25°C) | DMSO ≥ 45 mg/mL |
| Storage | 2-8°C, dry, sealed, protect from light |
| 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.
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