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  3. Cyclosporin A

Cyclosporin A  (Synonyms: Cyclosporine A; Ciclosporin A; CsA)

Cat. No.: HY-B0579 Purity: 99.97%
COA Handling Instructions

Cyclosporine A est un immunosuppresseur qui se lie à la cyclophiline et inhibe l'activité phosphatase de la calcineurine avec un IC50 de 5 nM. Cyclosporine A inhibe également l'adhésion CD11a/CD18.

Cyclosporin A ist ein Immunsuppressivum, das an das Cyclophilin bindet und die Phosphataseaktivität von Calcineurin mit einem IC50 von 5 nM hemmt. Cyclosporin A hemmt auch die CD11a/CD18-Adhäsion.

Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM. Cyclosporin A also inhibits CD11a/CD18 adhesion.

For research use only. We do not sell to patients.

Cyclosporin A Chemical Structure

Cyclosporin A Chemical Structure

CAS No. : 59865-13-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 111 publication(s) in Google Scholar

Other Forms of Cyclosporin A:

Top Publications Citing Use of Products

97 Publications Citing Use of MCE Cyclosporin A

Proliferation Assay
WB
IF

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142.  [Abstract]

    Representative western blotting images of cGAS and STING in the Cyclosporine (CsA; 10 μM; for 24 h)- or DMSO-treated NP cells.

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142.  [Abstract]

    Representative western blotting images of NLRP3, ASC, pro-CASP-1, cleaved CASP-1, GSDMD, and cleaved GSDMD in the (CsA; 10 μM; for 24 h)- or DMSO-treated NP cells.

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142.  [Abstract]

    Representative immunofluorescence images of STING with different degrees of polymerization in the Cyclosporine (CsA; 10 μM; for 24 h)- or DMSO-treated NP cells.

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Redox Biol. 2022 Aug;54:102355.

    Cells are treated with or without Cyclosporine A (CsA; 2 μM) for 4 h in presence of NRC-03 (45 μg/mL). Cell viability determined by CCK-8.

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Redox Biol. 2022 Aug;54:102355.

    Cells are treated with or without Cyclosporine A (CsA; 2 μM) for 4 h in presence of NRC-03 (45 μg/mL). TUNEL immunofluorescence staining and quantification of TUNEL positive cells.

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Aging Dis. 2022 Oct 1;13(5):1546-1561.  [Abstract]

    Additionally, similar to P-gp siRNA silence, pharmacological inhibition of P-gp with Cyclosporine A (CsA; 22 mg/kg) significantly attenuates P-gp expression levels in ischemic brain as compared to vehicle treatment.

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 May 18;12(1):2915.  [Abstract]

    Immunoblot analysis of Cytochrome c from cytosolic extracts and mitochondria from indicated cells pre-treated with DMSO or Cyclosporine A (50 μM) for 1 h, followed with PFOS treatment (150 μM, 6 h).

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Apr 20;12(5):413.  [Abstract]

    Inhibition of NR-induced increase of co-localized puncta (LC3 and TOM20) after 1 μMCyclosporin A (CsA) pretreatment.

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Apr 1;12(4):336.  [Abstract]

    Immunofluorescence staining of subcellular localization of NFATC1 in RANK overexpression and control cells with or without treatment of 10 μg/mL Cyclosporin A (CsA).

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Rep. 2021 Nov 30;37(9):110069.  [Abstract]

    Colony formation of CRC cells treated with Cyclosporine A (CsA; 2.5-5 μM) in combination with 5-FU or OXA for 48 h.

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Rep. 2021 Nov 30;37(9):110069.  [Abstract]

    Immunoblotting analysis of indicated apoptotic markers expression in CRC cells treated with Cyclosporine A (CsA; 2.5-5 μM) in combination with 5-FU or OXA.

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2021 Jan 12;118(2):e2009539118.  [Abstract]

    Calcineurin activities of the PCE after FK506 or Cyclosporine A (CsA; 4 µM) treatment Zebrafish.

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2021 Jun;178(11):2305-2323.  [Abstract]

    Smooth muscle cells are treated cyclosporin A (CsA, 1 μM) or PDTC (10 μM) for 24 h before measuring the activity of PPARγ2 promoter.

    Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):598.  [Abstract]

    A549 cells are pretreated with 5 µM Cyclosporin A (CSA) for 2 h, followed by treatment with 80 μM Hirsutine for 24 h. equal amount of lysates are subjected to immunoprecipitation using anti-ANT1 antibody, the associated CypD is determined using immunoblotting.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM[3]. Cyclosporin A also inhibits CD11a/CD18 adhesion[8].

    IC50 & Target

    IC50: 7 nM (calcineurin)

    In Vitro

    Cyclosporin A is able to bind with the cyclophilin in T cells[1].
    Cyclosporin A works by forming a Cyclophilin-Cyclosporin A complex to inhibit calcineurin[2].
    Cyclosporin A inhibits calcineurin in stimulated cells with an IC50 value of 7 nM[3].
    Cyclosporin A suppresses the nuclear translocation of NF-AT[4]. Cyclosporin A shows an effect on mitochondria via preventing the MTP from opening with an IC50 of 39 nM[5].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Cyclosporin A has immunosuppressive activity, and is active via parenteral and p.o. administration in mice, rat and guinea pigs[6].
    Cyclosporin A can be used in organ transplantation to prevent rejection[7].
    Pharmacokinetic parameters of blood showed area under the curve of 27.3 μg·h·mL-1, half-life of 6.9 h, volune of distribution of 3.7 L/kg in 140-200 g, 5-6 weeks, twelve adult male Wistar rats (Cyclosporin A 10 mg/kg; iv)[9].Blood pharmacokinetic parameters shows: Cyclosporin A (10 mg/kg; iv) has an area of the curve of 27.3 μg·h·mL-1 and a half-life of 6.9 h, and the distribution volume of 3.7 L/kg in male Wistar rats (140-200 g, 5-6 weeks)[9].

    1. Induction of Uraemia[10][11]
    Background
    Cyclosporin A administration induces interstitial deposition of collagen type III and fibrosis via stimulation of the Transforming Growth Factor beta (TGF-β)-signalling pathway, while inhibiting extracellular matrix (ECM) degradation via modulation of matrix metallopeptidase 9, thus leading to an imbalance in ECM turn over[2].
    Specific Mmodeling Methods
    Mice: Six-to-eight weeks old C57BL/6 mice
    Administration: 30 mg/kg • SC • daily for 16 weeks.
    Modeling Indicators
    Molecular changes: Upregulated mRNA expression of both LOX, LOXL2, TNFα, MCP-1, (NOX)4; significantly downregulated SOD2 mRNA expression; increased the urea nitrogen (BUN) level, increased tubular injury, interstitial inflammation and fibrosis scores, PAS scores, increased the level the deposition of collagen type I (COL1) and type III (COL3) in the renal ECM,increased the expression of alpha-smooth-muscle actin (α-SMA), fibronectin (FN), COL1A, MCP-1[10][11].
    Correlated Product(s):

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    1202.61

    Formula

    C62H111N11O12

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C/C=C/C[C@H]([C@@H](O)[C@@]1(N(C)C([C@]([H])(C(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@]([H])(CC(C)C)N(C)C([C@@H](C)NC([C@H](C)NC([C@@H](N(C([C@@]([H])(NC([C@@H](N(C(CN(C([C@@H](NC1=O)CC)=O)C)=O)C)CC(C)C)=O)C(C)C)=O)C)CC(C)C)=O)=O)=O)=O)=O)=O)[H])C

    Structure Classification
    Initial Source

    the fungus Beauveria nivea.

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 62.5 mg/mL (51.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 50 mg/mL (41.58 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.8315 mL 4.1576 mL 8.3152 mL
    5 mM 0.1663 mL 0.8315 mL 1.6630 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.62 mg/mL (2.18 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (1.73 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  Corn Oil

      Solubility: 20 mg/mL (16.63 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.97%

    References
    Cell Assay
    [3]

    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 50 μL 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 Kiker 52G 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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [6]

    Rats are immunized on day 0 i.p. with 0 5 mL and mice i.v. with 0 2 mL of a 10% suspension of washed sheep erythrocytes (SE). To elicit a secondary response, mice are boosted 8-11 weeks after the primary immunization with an i.v. injection of 0-2 mL of 0 25% washed SE (107 cells). For prolonged treatment the animals receive on the average 45 mg/kg cyclosporin A daily in the food during 13 weeks. These rats are immunized 5 days before killing.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 0.8315 mL 4.1576 mL 8.3152 mL 20.7881 mL
    5 mM 0.1663 mL 0.8315 mL 1.6630 mL 4.1576 mL
    10 mM 0.0832 mL 0.4158 mL 0.8315 mL 2.0788 mL
    15 mM 0.0554 mL 0.2772 mL 0.5543 mL 1.3859 mL
    20 mM 0.0416 mL 0.2079 mL 0.4158 mL 1.0394 mL
    25 mM 0.0333 mL 0.1663 mL 0.3326 mL 0.8315 mL
    30 mM 0.0277 mL 0.1386 mL 0.2772 mL 0.6929 mL
    40 mM 0.0208 mL 0.1039 mL 0.2079 mL 0.5197 mL
    DMSO 50 mM 0.0166 mL 0.0832 mL 0.1663 mL 0.4158 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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