Cyclosporin A structure
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Common Name | Cyclosporin A | ||
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CAS Number | 59865-13-3 | Molecular Weight | 1202.611 | |
Density | 1.0±0.1 g/cm3 | Boiling Point | 1293.8±65.0 °C at 760 mmHg | |
Molecular Formula | C62H111N11O12 | Melting Point | 148-151°C | |
MSDS | Chinese USA | Flash Point | 736.3±34.3 °C | |
Symbol |
GHS07, GHS08 |
Signal Word | Danger |
Use of Cyclosporin ACyclosporin A is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM. |
Name | cyclosporin A |
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Synonym | More Synonyms |
Description | Cyclosporin A is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM. |
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Related Catalog | |
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 exhibits inhibitory effect on calcineurin with an IC50 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]. |
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]. |
Kinase Assay | Reaction mixtures with purified enzyme contains 100 nM calcineurin, 100 nM calmodulin, and 5 μM 32P-labeled phosphopeptide, in 60 μL (total volume) of assay buffer containing 20 mM Tris (pH 8), 100 mM NaCl, 6 mM MgCl2, 0.5 mM dithiothreitol, 0.1 mg of bovine serum albumin per mL, and either 0.1 mM CaCl2 or 5 mM EGTA. Reaction mixtures with cell lysates contains 20 μL of undiluted lysate, 5 μM 32P-labeled phosphopeptide, and 40 μL of assay buffer. Reaction mixtures contains 50 μM peptide 412 or 413 and/or 500 nM okadaic acid, a specific inhibitor of phosphatases 1 and 2A; 500 nM okadaic acid is sufficient for inhibition of Ca2+-independent phosphatases, whereas higher concentrations partially inhibit Ca2+-dependent activity as well. After 15 min at 30°C, reactions are terminated by the addition of 0.5 mL of 100 mM potassium phosphate buffer (pH 7.0) containing 5% trichloroacetic acid. Free inorganic phosphate is isolated by Dowex cation-exchange chromatography and quantitated by scintillation counting as described. |
Cell Assay | 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 aprotinin 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. |
Animal Admin | 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. |
References |
Density | 1.0±0.1 g/cm3 |
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Boiling Point | 1293.8±65.0 °C at 760 mmHg |
Melting Point | 148-151°C |
Molecular Formula | C62H111N11O12 |
Molecular Weight | 1202.611 |
Flash Point | 736.3±34.3 °C |
Exact Mass | 1201.841309 |
PSA | 278.80000 |
LogP | 3.35 |
Vapour Pressure | 0.0±0.6 mmHg at 25°C |
Index of Refraction | 1.468 |
Storage condition | 2-8°C |
Water Solubility | ethanol: 30 mg/mL |
Cyclosporin A
Revision number: 5
SAFETY DATA SHEET Section1. IDENTIFICATION Product name:Cyclosporin A Revision number:5 Section2. HAZARDS IDENTIFICATION GHS classification PHYSICAL HAZARDSNot classified HEALTH HAZARDS Acute toxicity (Oral)Category 4 Category 1A Carcinogenicity Reproductive toxicityCategory 1B Reproductive toxicity (Effects on or via lactation) Additional category for effects on or via lactation ENVIRONMENTAL HAZARDSNot classified GHS label elements, including precautionary statements Pictograms or hazard symbols Signal wordDanger Hazard statementsHarmful if swallowed May cause cancer May damage fertility or the unborn child May cause harm to breast-fed children Precautionary statements: Obtain special instructions before use. [Prevention] Do not handle until all safety precautions have been read and understood. Do not breathe dust/fume/gas/mist/vapours/spray. Avoid contact during pregnancy/while nursing. Do not eat, drink or smoke when using this product. Wash hands thoroughly after handling. Use personal protective equipment as required. [Response]IF SWALLOWED: Call a POISON CENTER or doctor/physician if you feel unwell. Rinse mouth. IF exposed or concerned: Get medical advice/attention. [Storage]Store locked up. [Disposal]Dispose of contents/container through a waste management company authorized by the local government. Section3. COMPOSITION/INFORMATION ON INGREDIENTS Substance Substance/mixture: Cyclosporin A Section3. COMPOSITION/INFORMATION ON INGREDIENTS Components:Cyclosporin A Percent:>97.0%(LC)(N) CAS Number:59865-13-3 Synonyms:Cyclosporin Chemical Formula:C62H111N11O12 Section4. FIRST AID MEASURES Inhalation:Remove victim to fresh air and keep at rest in a position comfortable for breathing. Get medical advice/attention. Skin contact:Remove/Take off immediately all contaminated clothing. Gently wash with plenty of soap and water. Get medical advice/attention. Eye contact:Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Get medical advice/attention. Ingestion:Get medical advice/attention.Rinse mouth. Protection of first-aiders:A rescuer should wear personal protective equipment, such as rubber gloves and air- tight goggles. Section5. FIRE-FIGHTING MEASURES Suitable extinguishingDry chemical, foam, water spray, carbon dioxide. media: Specific hazards arising Take care as it may decompose upon combustion or in high temperatures to from the chemical:generate poisonous fume. Precautions for firefighters: Fire-extinguishing work is done from the windward and the suitable fire-extinguishing method according to the surrounding situation is used. Uninvolved persons should evacuate to a safe place. In case of fire in the surroundings: Remove movable containers if safe to do so. Special protectiveWhen extinguishing fire, be sure to wear personal protective equipment. equipment for firefighters: Section6. ACCIDENTAL RELEASE MEASURES Use extra personal protective equipment (P3 filter respirator for toxic particles). Keep Personal precautions, protective equipment and people away from and upwind of spill/leak. Entry to non-involved personnel should emergency procedures: be controlled around the leakage area by roping off, etc. Environmental precautions: Prevent product from entering drains. Methods and materials for Sweep dust to collect it into an airtight container, taking care not to disperse it. containment and cleaning Adhered or collected material should be promptly disposed of, in accordance with up: appropriate laws and regulations. Section7. HANDLING AND STORAGE Precautions for safe handling Technical measures:Handling is performed in a well ventilated place. Wear suitable protective equipment. Prevent dispersion of dust. Wash hands and face thoroughly after handling. Use a closed system if possible. Use a local exhaust if dust or aerosol will be generated. Advice on safe handling: Avoid all contact! Conditions for safe storage, including any incompatibilities Storage conditions:Keep container tightly closed. Store in a refrigerator. Store locked up. Store away from incompatible materials such as oxidizing agents. Heat-sensitive Comply with laws. Packaging material: Section8. EXPOSURE CONTROLS / PERSONAL PROTECTION Engineering controls:Install a closed system or local exhaust. Also install safety shower and eye bath. Cyclosporin A Section8. EXPOSURE CONTROLS / PERSONAL PROTECTION Personal protective equipment Respiratory protection: Dust respirator, self-contained breathing apparatus(SCBA), supplied air respirator, etc. Use respirators approved under appropriate government standards and follow local and national regulations. Hand protection:Impervious gloves. Safety goggles. A face-shield, if the situation requires. Eye protection: Skin and body protection: Impervious protective clothing. Protective boots, if the situation requires. Section9. PHYSICAL AND CHEMICAL PROPERTIES Physical state (20°C):Solid Crystal- Powder Form: Colour:White - Almost white No data available Odour: pH: No data available Melting point/freezing point:151°C Boiling point/range:No data available Flash point:No data available Flammability or explosive limits: Lower:No data available Upper:No data available Relative density:No data available Solubility(ies): [Water]No data available [Other solvents] Very soluble:Methanol, Ether, Acetone, Ethanol Soluble:Chloroform Log Pow:2.92 Section10. STABILITY AND REACTIVITY Chemical stability:Stable under proper conditions. Possibility of hazardous No special reactivity has been reported. reactions: Incompatible materials: Oxidizing agents Hazardous decomposition Carbon monoxide, Carbon dioxide, Nitrogen oxides (NOx) products: Section11. TOXICOLOGICAL INFORMATION Acute Toxicity:orl-rat LD50:1480 mg/kg ipr-rat LD50:147 mg/kg scu-rat LD50:286 mg/kg ivn-rat LD50:24 mg/kg Skin corrosion/irritation: No data available Serious eyeNo data available damage/irritation: Germ cell mutagenicity: sce-hmn-lym 1 mg/L oms-hmn-lym 50 mg/L Carcinogenicity:orl-man TDLo:259 mg/kg/2W-C IARC =Group 1 (Carcinogenic to humans) NTP =a (Known to be carcinogens) No data available Reproductive toxicity: RTECS Number:GZ4120000 Section12. ECOLOGICAL INFORMATION Ecotoxicity: Fish:No data available Crustacea:No data available Cyclosporin A Section12. ECOLOGICAL INFORMATION Algae:No data available Persistence / degradability: No data available BioaccumulativeNo data available potential(BCF): Mobility in soil 2.92 Log Pow: Soil adsorption (Koc):No data available No data available Henry's Law constant(PaM3/mol): Section13. DISPOSAL CONSIDERATIONS Recycle to process, if possible. Consult your local regional authorities. You may be able to dissolve or mix material with a combustible solvent and burn in a chemical incinerator equipped with an afterburner and scrubber system. Observe all federal, state and local regulations when disposing of the substance. Section14. TRANSPORT INFORMATION Does not correspond to the classification standard of the United Nations Hazards Class: UN-No:Not listed Section15. REGULATORY INFORMATION Safe management ordinance of dangerous chemical product (State Council announces on January 26, 2002 and revised on February 16,2011): Safe use and production, the storage of a dangerous chemical, transport, loading and unloading were prescribed. SECTION 16 - ADDITIONAL INFORMATION N/A |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
MUTATION DATA
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Symbol |
GHS07, GHS08 |
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Signal Word | Danger |
Hazard Statements | H302-H350-H360 |
Precautionary Statements | P201-P301 + P312 + P330-P308 + P313 |
Personal Protective Equipment | Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges |
Hazard Codes | T:Toxic |
Risk Phrases | R45;R60;R22 |
Safety Phrases | 53-45-36/37-24/25-22 |
RIDADR | NONH for all modes of transport |
WGK Germany | 3 |
RTECS | GZ4120000 |
HS Code | 2941909000 |
Precursor 0 | |
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DownStream 2 | |
HS Code | 2941909000 |
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