Cyclosporin A
- CAS No.
- 59865-13-3
- Chemical Name:
- Cyclosporin A
- Synonyms
- CYCLOSPORINE;CICLOSPORIN;CYCLOSPORINE A;Restasis;sandimmune;Neoral;CICLOSPORIN A;CL285;Cipol N;s7481f1
- CBNumber:
- CB5163816
- Molecular Formula:
- C62H111N11O12
- Molecular Weight:
- 1202.61
- MOL File:
- 59865-13-3.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/5/8 14:18:51
Melting point | 148-151°C |
---|---|
Boiling point | 838.63°C (rough estimate) |
alpha | D20 -244° (c = 0.6 in chloroform); D20 -189° (c = 0.5 in methanol) |
Density | 0.9913 (rough estimate) |
refractive index | 1.6500 (estimate) |
Flash point | 87℃ |
storage temp. | -20°C |
solubility | ethanol: 30 mg/mL |
form | solid |
pka | 13.32±0.70(Predicted) |
color | white |
Water Solubility | Soluble in dimethyl sulfoxide and ethanol. Insoluble in water. |
Merck | 14,2752 |
BRN | 3647785 |
Stability | Stable for 3 years as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
InChIKey | PMATZTZNYRCHOR-CGLBZJNRSA-N |
CAS DataBase Reference | 59865-13-3(CAS DataBase Reference) |
IARC | 1 (Vol. 50, 100A) 2012 |
EPA Substance Registry System | Cyclosporin A (59865-13-3) |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07,GHS08 |
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Signal word | Danger | |||||||||
Hazard statements | H302-H350-H360FD | |||||||||
Precautionary statements | P201-P202-P264-P270-P301+P312-P308+P313 | |||||||||
Hazard Codes | T,Xn,F | |||||||||
Risk Statements | 45-60-22-40-36-20/21/22-11 | |||||||||
Safety Statements | 53-45-36/37-24/25-22-26-16 | |||||||||
RIDADR | UN 1648 3 / PGII | |||||||||
WGK Germany | 3 | |||||||||
RTECS | GZ4120000 | |||||||||
HS Code | 29419090 | |||||||||
Toxicity | LD50 in mice, rats, rabbits (mg/kg): 107, 25, >10 i.v.; 2329, 1480, >1000 orally (Ryffel) | |||||||||
NFPA 704 |
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Cyclosporin A price More Price(12)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich(India) | SML1018 | Cyclosporin A, Ready Made Solution 1?mg/mL in DMSO | 59865-13-3 | 1ML | ₹13020.7 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | PHR1092 | Cyclosporine Pharmaceutical Secondary Standard; Certified Reference Material | 59865-13-3 | 500MG | ₹15144.18 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | C3662 | Cyclosporin A from Tolypocladium inflatum, ≥95% (HPLC), solid | 59865-13-3 | 5MG | ₹20567.5 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | C3662 | Cyclosporin A from Tolypocladium inflatum, ≥95% (HPLC), solid | 59865-13-3 | 10MG | ₹34542.58 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | C1832 | Cyclosporin A from Tolypocladium inflatum, BioReagent, for molecular biology, ≥95% | 59865-13-3 | 5MG | ₹26954.25 | 2022-06-14 | Buy |
Cyclosporin A Chemical Properties,Uses,Production
Description
Cyclosporine A is a powerful immunosuppressive drug intended for preventing rejection
of kidney, heart, and lung transplants.
A new era in the development of immunopharmacology began with the discovery of
cyclosporines.
Cyclosporines are produced by mycelial mushrooms Tolypocladium inflatum,
Tricoderma polysporum, and Cylindrocarpon lucidum, which are found in the ground.
Cyclosporine A is the first drug to affect a specific line of protecting cells of the body.
Unlike usual cytotoxics, it suppresses T-cells and acts on all cell lines simultaneously.
Cyclosporine A significantly eases the ‘reception’ of transplants, and increases the possibility of treating autoimmune system diseases.
Chemical Properties
White or almost white powder
Uses
Cyclosporin A is a hydrophobic cyclic peptide isolated from several fungal species including Cylindrocarpon, Fusarium, Trichoderma and Tolypocladium. Cyclosporin A inhibits T-cell activation and has been marketed since 1983 as an immunosuppressant in post-allogeneic organ transplant. Cyclosporin A acts by binding to the protein, cyclophilin (immunophilin), in T-lymphocytes causing inhibition of calcineurin (protein phosphatase 2B). Cyclosporin A reduces transcription of interleukin 2, and inhibits lymphokine production, interleukin release and NO synthesis induced by interleukin 1α, lipopolysaccharides and TNFα.
Definition
ChEBI: A cyclic nonribosomal peptide of eleven amino acids; an immunosuppressant drug widely used in post-allogeneic organ transplant to reduce the activity of the patient's immune system, and therefore the risk of organ rejection. Also causes reversible inhibiti n of immunocompetent lymphocytes in the G0- and G1-phase of the cell cycle.
Indications
General Description
White prismatic needles (from acetone) or white powder.
Air & Water Reactions
Slightly water soluble .
Reactivity Profile
Cyclosporin A is an amide. Amides/imides react with azo and diazo compounds to generate toxic gases. Flammable gases are formed by the reaction of organic amides/imides with strong reducing agents. Amides are very weak bases (weaker than water). Imides are less basic yet and in fact react with strong bases to form salts. That is, they can react as acids. Mixing amides with dehydrating agents such as P2O5 or SOCl2 generates the corresponding nitrile. The combustion of these compounds generates mixed oxides of nitrogen (NOx).
Health Hazard
SYMPTOMS: Symptoms of exposure to Cyclosporin A include hepatotoxicity, nephrotoxicity, hyperkalemia, hyperuricemia, convulsions, renal dysfunction, tremor, hirsutism, hypertension, gum hyperplasia, cramps, acne, headache, diarrhea, nausea, vomiting, abdominal discomfort, paresthesia, flushing, leukopenia, lymphoma, sinusitis and gynecomastia. In 2% or less of persons exposed, it has caused allergic reactions, anemia, anorexia, confusion, conjunctivitis, edema, fever, brittle fingernails, gastritis, hearing loss, hiccups, hyperglycemia, muscle pain, peptic ulcer, thrombocytopenia and tinnitus. Rare reactions include anxiety, chest pain, constipation, depression, hair breaking hematuria, joint pain, lethargy, mouth sores, myocardial infarction, night sweats, pancreatitis, pruritus, swallowing difficulty, tingling, upper gastrointestinal bleeding, visual disturbance, weakness and weight loss. It has caused kidney and liver damage. An increased susceptibility to infection may occur. Other symptoms include gastrointestinal disturbance, rashes and angioedema.
Fire Hazard
Flash point data for Cyclosporin A are not available; however, Cyclosporin A is probably combustible.
Pharmacology
Cyclosporine has no direct effect on keratinocytes and is not a mitotic inhibitor. Cyclosporine inhibits cytokine release, which results in a decreased recruitment of APCs into the epidermis and decreases immunoreactivity of lesions. Potential long-term side effects preclude cyclosporine’s use in all but very severe and recalcitrant psoriasis. Cyclosporine can be combined with lowdose methotrexate.
Side effects
Cyclosporine’s main side effects, even at low doses, are hypertension and nephrotoxicity. Age, baseline blood pressure, and baseline creatinine levels are predictors of higher risks of side effects. Glomerular filtration rate (GFR) is a more sensitive test than creatinine for evaluating renal function, and a baseline is recommended in any high-risk patient. Longterm treatment with CSA may induce interstitial fibrosis and glomerular sclerosis, with more pronounced changes directly associated with duration of therapy. It should be administered only by dermatologists experienced in its use.
Safety Profile
Confirmed carcinogen producing Hodghn's dlsease. Experimental reproductive effects. Poison by intraperitoneal and intravenous routes. Moderately toxic by ingestion. Human systemic effects by ingestion: increased body temperature, cyanosis. Mutation data reported. When heated to decomposition it emits toxic fumes of NOx.
Potential Exposure
Cyclosporin A is a fungal metabolite; an amide immunosuppressant drug used in various surgeries.
Carcinogenicity
Cyclosporin A is known to be a human carcinogen based on sufficient evidence of carcinogenicity from studies in humans.
Shipping
UN3249 Medicine, solid, toxic, n.o.s., Hazard Class: 6.1; Labels: 6.1-Poisonous materials.
Incompatibilities
Amides/imides react with azo and diazo compounds to generate toxic gases. Flammable gases are formed by the reaction of organic amides/imides with strong reducing agents such as hydrideds and active metals. Amides are very weak bases (weaker than water). Imides are less basic yet and in fact react with strong bases to form salts. That is, they can react as acids. Mixing amides with dehydrating agents such as such as phosphorus pent- oxide or thionyl chloride generates the corresponding nitrile. The combustion of these compounds generates mixed oxides of nitrogen (NOx).
Waste Disposal
t is inappropriate and possibly dangerous to the environment to dispose of expired or waste drugs and pharmaceuticals by flushing them down the toilet or discarding them to the trash. Household quantities of expired or waste pharmaceuticals may be mixed with wet cat litter or coffee grounds, double-bagged in plastic, discard in trash. Larger quantities shall carefully take into consider- ation applicable DEA, EPA, and FDA regulations. If possi- ble return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged, and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.
Cyclosporin A Preparation Products And Raw materials
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
Clickchem Research LLP | +91-8140031133 +91-8140031133 | Gujarat, India | 411 | 58 | Inquiry |
Novas International | 91--7600004306 | Gujarat, India | 210 | 58 | Inquiry |
HiMedia Laboratories | 91-22-61471919 | Maharashtra, India | 1843 | 58 | Inquiry |
Maas Pharma Chemicals | +91-9958666224 | Delhi, India | 1607 | 58 | Inquiry |
Newedge Overseas | 91-79-40307106 | Gujarat, India | 109 | 58 | Inquiry |
Thykn (India) International | 91-22-67033666 | Maharashtra, India | 89 | 58 | Inquiry |
Mulji Mehta Pharma | 08048372632Ext 619 | Mumbai, India | 134 | 58 | Inquiry |
Pharma Affiliates | 172-5066494 | Haryana, India | 6761 | 58 | Inquiry |
Cytochrome Life Sciences Pvt., Ltd. | 91-11-42147939 | Delhi, India | 17 | 58 | Inquiry |
Atlanta Associates | 08048372939Ext 940 | Mumbai, India | 184 | 58 | Inquiry |
Supplier | Advantage |
---|---|
Clickchem Research LLP | 58 |
Novas International | 58 |
HiMedia Laboratories | 58 |
Maas Pharma Chemicals | 58 |
Newedge Overseas | 58 |
Thykn (India) International | 58 |
Mulji Mehta Pharma | 58 |
Pharma Affiliates | 58 |
Cytochrome Life Sciences Pvt., Ltd. | 58 |
Atlanta Associates | 58 |
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