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[CAS NO. 59865-13-3]  Cyclosporin A

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PRODUCTS SPECIFICATIONS [59865-13-3]

Catalog
HY-B0579
Brand
MCE
CAS
59865-13-3

DESCRIPTION [59865-13-3]

Overview

MDLMFCD00274558
Molecular Weight1202.61
Molecular FormulaC62H111N11O12
SMILESC/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

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

71 Publications Citing Use of MCE


Summary

Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC 50 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 IC 50 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 IC 50 of 39 nM [5] .

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] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT04412785 University of Pennsylvania
COVID-19
June 30, 2020 Phase 1
NCT01370343 Pfizer
Healthy|Drug Interaction
July 2011 Phase 1
NCT00548301 Sirion Therapeutics, Inc.
Dry Eye Syndromes
Phase 3

Appearance

Solid


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)

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
10 mM 0.0832 mL 0.4158 mL 0.8315 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: corn oil

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

  • 2.

    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

  • 3.

    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

  • 4.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

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

  • 5.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.08 mg/mL (1.73 mM); Clear solution

* All of the co-solvents are available by MCE.


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