Cyclosporin A |
| Catalog No.GC13941 |
Cyclosporin A is an immunosuppressive agent which has three major cellular targets including cyclophilins, calcineurin and transporters while it can inhibit the activity of cyclophilin A and calcineurin with an IC50 of 360nM and 5nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 59865-13-3
Sample solution is provided at 25 µL, 10mM.
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Cyclosporin A is an immunosuppressive agent which has three major cellular targets including cyclophilins, calcineurin and transporters[1] while it can inhibit the activity of cyclophilin A and calcineurin with an IC50 of 360nM[1] and 5nM[2]. Cyclosporin A-mediated immunosuppression is achieved by forming a ternary complex with cyclophilins and calcineurin to block the phosphatase activity of calcineurin and thus dephosphorylation and nuclear shuttling of the nuclear factor of activated T-cells (NFAT) is inhibited [1, 3]. Cyclosporine A is mainly used in clinical practice to inhibit immune failure in xenograft tissues [1].
Cyclosporin A (0.001nM~1mM; 24h) inhibited production of IL-2 in Jurkat cells stimulated with OKT3 monoclonal antibody and PMA (phorbol 12-myristate 13-acetate) with an IC50 of 10nM [2]; Cyclosporin A (4μM; 18h) reduced viral envelope protein secretion from hepatitis B virus-infected HepaRG cells [1]; Cyclosporin A (10μM; 24h) reduced viral gene expression and viral titers significantly in human bronchial epithelial cells (HBEpCs) infected with SARS-CoV-2 [4].
Cyclosporin A (50mg/kg; 6d; p.o.) reduced viral RNA in Balb/c mice infected with SARS-CoV-2 [4]; Cyclosporin A (10mg/kg; 2d/tid.; p.o.) significantly reduced the accumulation of eosinophils in the lung of male Hartley guinea-pig which were sensitized by ovalbumin [5]; Cyclosporin A (5mg/kg; 3weeks; p.o.) increased the serum creatinine and blood urea nitrogen (BUN) levels in male Wistar rats [6].
References:
[1] Watashi K, Sluder A, Daito T, et al. Cyclosporin A and its analogs inhibit hepatitis B virus entry into cultured hepatocytes through targeting a membrane transporter, sodium taurocholate cotransporting polypeptide (NTCP) [J]. Hepatology, 2014, 59(5): 1726-1737.
[2] Fruman D A, Klee Cb F-Bierer B E, Bierer Be F-Burakoff S J, et al. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A [J]. Proceedings of the National Academy of Sciences of the United States of America, 1992, 89(9): 3686-3690.
[3] Schiene-Fischer C, Fischer G, Braun M, et al. Non-immunosuppressive cyclophilin inhibitors [J]. Angewandte Chemie, 2022, 61(39): e202201597.
[4] Sauerhering L, Kuznetsova I, Kupke A, et al. Cyclosporin A reveals potent antiviral effects in preclinical models of SARS-CoV-2 Infection [J]. American Journal of Respiratory and Critical Care Medicine, 2022, 205(8): 964-968.
[5] Lagente V, Carré C, Kyriacopoulos F, et al. Inhibitory effect of cyclosporin A on eosinophil infiltration in the guinea-pig lung induced by antigen, platelet-activating factor and leukotriene B4 [J]. The European Respiratory Journal, 1994, 7(5): 921-926.
[6] Sereno J, Rodrigues-Santos P, Vala H, et al. Transition from cyclosporine-induced renal dysfunction to nephrotoxicity in an in vivo rat model [J]. International journal of molecular sciences, 2014, 15(5): 8979-8997.
| Cell experiment [1]: | |
Cell lines | Jurkat cells |
Preparation Method | Cells were stimulated with OKT3 monoclonal antibody (1:4000 dilution of ascites) and 2ng of PMA (phorbol 12-myristate 13-acetate) per ml for 24h in the presence of different concentrations of Cyclosporin A (absence of Cyclosporin A as a control). |
Reaction Conditions | 0.001nM~1mM; 24h |
Applications | Cyclosporin A inhibited production of IL-2. |
| Animal experiment [2]: | |
Animal models | Male Wistar rats |
Preparation Method | The rats were fed with Cyclosporin A (5 mg/kg) for 3 weeks and the vehicle as a control. The concentrations of creatinine and blood urea nitrogen (BUN) in serum were determined as indexes for evaluating renal function. |
Dosage form | 5mg/kg; 3weeks; p.o. |
Applications | Cyclosporin A increased the serum creatinine and BUN levels. |
References: | |
| Cas No. | 59865-13-3 | SDF | |
| Canonical SMILES | CCC1C(=O)N(CC(=O)N(C(C(=O)NC(C(=O)N(C(C(=O)NC(C(=O)NC(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N1)C(C(C)CC=CC)O)C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C | ||
| Formula | C62H111N11O12 | M.Wt | 1202.61 |
| Solubility | ≥ 60.15mg/mL in DMSO | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 831.5 μL | 4.1576 mL | 8.3152 mL |
| 5 mM | 166.3 μL | 831.5 μL | 1.663 mL |
| 10 mM | 83.2 μL | 415.8 μL | 831.5 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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