Cyclosporine (NSC-290193)

Catalog No.S1514

For research use only.

Cyclosporine (NSC-290193) is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.

Cyclosporine (NSC-290193) Chemical Structure

CAS No. 79217-60-0

Selleck's Cyclosporine (NSC-290193) has been cited by 11 Publications

Purity & Quality Control

Choose Selective phosphatase Inhibitors

Biological Activity

Description Cyclosporine (NSC-290193) 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)

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

3mg/mL

Chemical Information

Molecular Weight 1202.61
Formula

C62H111N11O12

CAS No. 79217-60-0
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg 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.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04989686 Withdrawn Other: Microsampling Immunosuppression Children''s Hospital of Philadelphia March 2022 --
NCT05202145 Completed Drug: ALXN2050|Drug: Cyclosporine|Drug: Tacrolimus|Drug: MMF Healthy Alexion Pharmaceuticals January 11 2022 Phase 1
NCT05056779 Withdrawn Drug: Nemolizumab|Drug: CD14152 placebo Moderate-to-severe Atopic Dermatitis Galderma R&D January 2022 Phase 3
NCT04988256 Enrolling by invitation Drug: Cyclosporine|Drug: Methylprednisolone and Prednisone DRESS Syndrome|Drug-Induced Hypersensitivity Syndrome University of Southern California September 27 2021 Early Phase 1
NCT04542252 Completed Drug: SyB V-1901|Drug: Cyclosporine Drug Drug Interaction SymBio Pharmaceuticals November 9 2020 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
What is the difference between S2286 (cyclosporin A) and S1514 (cyclosporin)?

Answer:
Cyclosporine is a mixture of Cyclosporine A, derivatives of Cyclosporine A, salts of Cyclosporine A. Cyclosporine A is an especially useful Cyclosporine component.

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