Cyclosporine

Catalog No.S1514 Batch:S151406

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Technical Data

Formula

C62H111N11O12

Molecular Weight 1202.61 CAS No. 79217-60-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (83.15 mM)
Ethanol 100 mg/mL (83.15 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
2%DMSO 40%PEG300 2%Tween80 56%ddH2O
3.0mg/ml Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 560 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.
Targets
calcineurin phosphatase [2]
In vitro Cyclosporine induces phenotypic changes, including invasiveness of non-transformed cells, by a cell-autonomous mechanism. Cyclosporine treatment of adenocarcinoma cells results in striking morphological alterations, including membrane ruffling and numerous pseudopodial protrusions, increased cell motility, and anchorage-independent (invasive) growth. [1] Cyclosporine (cyclosporin A, CsA) has potent immunosuppressive properties, reflecting its ability to block the transcription of cytokine genes in activated T cells. Cyclosporine through formation of a complex with cyclophilin inhibits the phosphatase activity of calcineurin, which regulates nuclear translocation and subsequent activation of NFAT transcription factors. Cyclosporine also blocks the activation of JNK and p38 signaling pathways triggered by antigen recognition, making CsA a highly specific inhibitor of T cell activation. [2] Cyclosporine-mediated inhibition of the biliary excretion of MPAG by the Mrp2 transporter is the mechanism responsible for the interaction between Cyclosporine and mycophenolate mofetil (MMF). [3] Cyclosporine inhibits biochemical and morphological differentiation of skeletal muscle cells while having a minimal effect on proliferation. [4]
In vivo Cyclosporine enhances tumour growth in immunodeficient SCID-beige mice. [1] Cyclosporine inhibits muscle regeneration after induced trauma in mice. [4] Cyclosporine peaks at 1 hour in blood, spleen, and kidney, with higher concentrations in spleen and kidney than in blood. [5]

Protocol (from reference)

Selleck's Cyclosporine has been cited by 14 publications

TRPM2-mediated feed-forward loop promotes chondrocyte damage in osteoarthritis via calcium-cGAS-STING-NF-κB pathway [ J Adv Res, 2024, S2090-1232(24)00499-5] PubMed: 39505144
ATP/IL-33-Co-Sensing by Mast Cells (MCs) Requires Activated c-Kit to Ensure Effective Cytokine Responses [ Cells, 2023, 12(23)2696] PubMed: 38067124
Masitinib Inhibits Hepatitis A Virus Replication [ Int J Mol Sci, 2023, 24(11)9708] PubMed: 37298659
Bacterial infection reinforces host metabolic flux from arginine to spermine for NLRP3 inflammasome evasion [ Cell Rep, 2021, 34(10):108832] PubMed: 33691113
Combination of ponatinib with deferoxamine synergistically mitigates ischemic heart injury via simultaneous prevention of necroptosis and ferroptosis [ Eur J Pharmacol, 2021, 898:173999] PubMed: 33675785
Transportin-1 binds to the HIV-1 capsid via a nuclear localization signal and triggers uncoating. [ Nat Microbiol, 2019, 4(11):1840-1850] PubMed: 31611641
Inhibition of MDR1 overcomes resistance to brentuximab vedotin in Hodgkin lymphoma. [ Clin Cancer Res, 2019, clincanres.1768.2019] PubMed: 31811017
A targeted genomic alteration analysis predicts survival of melanoma patients under BRAF inhibitors [ Oncotarget, 2019, 10(18):1669-1687] PubMed: 30899440
Topical application of phenytoin or nifedipine-loaded PLGA microspheres promotes periodontal regeneration in vivo. [ Arch Oral Biol, 2019, 97:42-51] PubMed: 30342306
[ Theranostics, 2018, ] PubMed: 30083255

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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