Азатиоприн
- английское имяAzathioprine
- CAS №446-86-6
- CBNumberCB2170327
- ФормулаC9H7N7O2S
- мольный вес277.26
- EINECS207-175-4
- номер MDLMFCD00069203
- файл Mol446-86-6.mol
химическое свойство
| Температура плавления | 243-244°C |
| Температура кипения | 521.0±60.0 °C(Predicted) |
| плотность | 1.5379 (rough estimate) |
| показатель преломления | 1.7400 (estimate) |
| температура хранения | 2-8°C |
| растворимость | Soluble in Dichloromethane and dimethyl sulfoxide. |
| пка | 8.2(at 25℃) |
| форма | Solid |
| цвет | Pale-yellow crystals from Me2CO (aq) |
| Биологические источники | synthetic (organic) |
| Растворимость в воде | <0.1 g/100 mL at 23 ºC |
| Мерк | 14,902 |
| BCS Class | 4 |
| Стабильность | Stable. Incompatible with strong oxidizing agents, strong bases. |
| ИнЧИКей | LMEKQMALGUDUQG-UHFFFAOYSA-N |
| Справочник по базе данных CAS | 446-86-6(CAS DataBase Reference) |
| FDA UNII | MRK240IY2L |
| МАИР | 1 (Vol. 26, Sup 7, 100A) 2012 |
| Предложение 65 Список | Azathioprine |
| Словарь наркотиков NCI | Imuran |
| Код УВД | L04AX01 |
| Система регистрации веществ EPA | Azathioprine (446-86-6) |
| UNSPSC Code | 41116107 |
| NACRES | NA.77 |
больше
| Коды опасности | Xi,T,Xn | |||||||||
| Заявления о рисках | 45-22-36/37/38-20/21/22 | |||||||||
| Заявления о безопасности | 53-22-26-36/37-45-36 | |||||||||
| WGK Германия | 3 | |||||||||
| RTECS | UO8925000 | |||||||||
| Класс опасности | IRRITANT | |||||||||
| кода HS | 29339900 | |||||||||
| Банк данных об опасных веществах | 446-86-6(Hazardous Substances Data) | |||||||||
| Токсичность | LD50 orl-rat: 535 mg/kg NIIRDN 6,3,82 | |||||||||
| NFPA 704: |
|
рисовальное письмо(GHS)
-
рисовальное письмо(GHS)
-
сигнальный язык
опасность
-
вредная бумага
H315：При попадании на кожу вызывает раздражение.
H319：При попадании в глаза вызывает выраженное раздражение.
H335：Может вызывать раздражение верхних дыхательных путей.
H302：Вредно при проглатывании.
H350：Может вызывать раковые заболевания.
H361fd：Предполагается, что данное вещество может отрицательно повлиять на способность к деторождению. Предполагается, что данное вещество может отрицательно повлиять на неродившегося ребенка.
-
оператор предупредительных мер
P202：Перед использованием ознакомиться с инструкциями по технике безопасности.
P261：Избегать вдыхания пыли/ дыма/ газа/ тумана/ паров/ аэрозолей.
P301+P312：ПРИ ПРОГЛАТЫВАНИИ: Обратиться за медицинской помощью при плохом самочувствии.
P302+P352：ПРИ ПОПАДАНИИ НА КОЖУ: Промыть большим количеством воды.
P305+P351+P338：ПРИ ПОПАДАНИИ В ГЛАЗА: Осторожно промыть глаза водой в течение нескольких минут. Снять контактные линзы, если Вы ими пользуетесь и если это легко сделать. Продолжить промывание глаз.
P308+P313：ПРИ подозрении на возможность воздействия обратиться за медицинской помощью.
Азатиоприн химические свойства, назначение, производство
Описание
This immunosuppressive and antineoplastic drug is derived from 6-mercaptopurine. It caused occupational dermatitis in a pharmaceutical worker, reconditioner of old tablet packaging machines and in a production mechanic, working in packaging for a pharmaceutical company.Химические свойства
Azathioprine is a complex heterocyclic compound which forms pale yellow crystals.Использование
An immunosuppressive antimetabolite. Also active as disease modifying antirheumatic drug (DMARD). Azathioprine is a purine analog with immunosuppressive effects.Определение
ChEBI: A thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and a ter organ transplantation and also for treatment of Crohn's didease and MS.Показания
Azathioprine (Imuran) is a cytotoxic agent that preferentially destroys any rapidly dividing cell. Since immunologically competent cells are generally rapidly dividing cells, azathioprine is very effective as an immunosuppressive drug. Unfortunately, any cell that is replicating is a target for this action. This lack of specificity leads to serious side effects. Azathioprine, in combination with corticosteroids, has historically been used more widely than any other drug in immunosuppressive therapy. It is classified as a purine antimetabolite and is a derivative of 6-mercaptopurine.Общее описание
Pale yellow crystals or yellowish powder. Decomposes at 243-244°C. Used for the treatment of rheumatoid arthritis. A known carcinogen.Реакции воздуха и воды
Sensitive to oxidation in the air. Insoluble in water.Профиль реактивности
Azathioprine may react exothermically with acids. Incompatible with isocyanates, peroxides, phenols, epoxides, anhydrides, and acid halides. Hydrolyzed by strongly basic solutions . May react with strong reducing agents to generate flammable gaseous hydrogen or hydrogen sulfide.Опасность
Confirmed carcinogen.Пожароопасность
Flash point data for Azathioprine are not available. Azathioprine is probably combustible.Контактные аллергены
This immunosuppressive and antineoplastic drug is derived from 6-mercaptopurine. It caused allergic contact dermatitis in a mother crushing tablets for her leukemic son, and occupational dermatitis in a pharmaceutical reconditioner of old tablet packaging machines, and in a production mechanic working in packaging for a pharmaceutical company.Механизм действия
Azathioprine is a phase-specific drug that is toxic to cells during nucleic acid synthesis. Phase-specific drugs are toxic during a specific phase of the mitotic cycle, usually the S-phase, when DNA synthesis is occurring, as opposed to cycle-specific drugs that kill both cycling and intermitotic cells.Azathioprine is converted in vivo to thioinosinic acid, which competitively inhibits the synthesis of inosinic acid, the precursor to adenylic acid and guanylic acid. In this way, azathioprine inhibits DNA synthesis and therefore suppresses lymphocyte proliferation.This effectively inhibits both humoral and cell-mediated immune responses.
Фармаколо?гия
Azathioprine is well absorbed following oral administration, with peak blood levels occurring within 1 to 2 hours. It is rapidly and extensively metabolized to 6- mercaptopurine, which is further converted in the liver and erythrocytes to a variety of metabolites, including 6- thiouric acid. Metabolites are excreted in the urine.The half-life of azathioprine and its metabolites in the blood is about 5 hours.Клиническое использование
Azathioprine is a relatively powerful antiinflammatory agent. Although its beneficial effect in various conditions is principally attributable to its direct immunosuppressive action, the antiinflammatory properties of the drug play an important role in its overall therapeutic effectiveness.Azathioprine has been used widely in combination with corticosteroids to inhibit rejection of organ transplants, particularly kidney and liver allografts. However, it is usually reserved for patients who do not respond to cyclosporine plus corticosteroids alone.
Azathioprine also has applications in certain disorders with autoimmune components, most commonly rheumatoid arthritis. It is as effective as cyclophosphamide in the treatment of Wegener’s granulomatosis. It has largely been replaced by cyclosporine in immunosuppressive therapy. Relative to other cytotoxic agents, the better oral absorption of azathioprine is the reason for its more widespread clinical use.
Побочные эффекты
The therapeutic use of azathioprine has been limited by the number and severity of adverse effects associated with its administration. Bone marrow suppression resulting in leukopenia, thrombocytopenia, or both may occur. GI toxicity may be a problem. It is also mildly hepatotoxic. Because of its immunosuppressive activity, azathioprine therapy can lead to serious infections. It has been shown to be mutagenic in animals and humans and carcinogenic in animals.Профиль безопасности
Confirmed human carcinogen producing bladder tumors and leukemia. Poison by subcutaneous, intradermal, and intraperitoneal routes. Moderately toxic by ingestion. Human systemic effects: liver changes, hypermotility, diarrhea, nausea or vomiting, increased body temperature, BP lowering, decreased urine volume or anuria, normocytic anemia, bone marrow changes. An experimental teratogen. Other experimental reproductive effects. Human mutation data reported. When heated to decomposition it emits very toxic fumes of NO,xand SOx. An immunosuppressant.Возможный контакт
Azathioprine is an immunosuppressive agent, generally used in combination with a corticosteroid to prevent rejection following renal homotransplantations. It also is used following transplantation of other organs. Other uses of azathioprine include the treatment of a variety of presumed autoimmune diseases, including rheumatoid arthritis; ankylosing spondylitis; systemic lupus erythematosus; dermatonyositis, periarteritis nodosa, scleroderma, refractory thombocytopenic purpura; autoimmune hemolytic anemia; chronic active liver disease; regional enteritis; ulcerative colitis; various autoimmune diseases of the eye; acute and chronic glomerulonephritis; the nephritic syndrome; Wegener’s granulomatosis; and multiple sclerosis.Канцерогенность
Azathioprine is known to be a human carcinogen based on sufficient evidence of carcinogenicity from studies in humans.Перевозки
UN2811 Toxic solids, organic, n.o.s., Hazard Class: 6.1; Labels: 6.1-Poisonous materials, Technical Name Required.Несовместимости
Incompatible with reducing agents, such as hydrides (may cause the release of explosive gases), oxidizers (chlorates, nitrates, peroxides, permanganates, perchlorates, chlorine, bromine, fluorine, etc.); contact may cause fires or explosions. Keep away from alkaline materials, strong acids (violent exothermic reaction), strong bases.Азатиоприн запасные части и сырье
Азатиоприн поставщик
| поставщик | телефон | страна | номенклатура продукции | благоприятные условия |
|---|---|---|---|---|
| +86-13131129325 | China | 5887 | 58 | |
| +8617732866630 | China | 18147 | 58 | |
| +8618092446649 | China | 1143 | 58 | |
| +86-（0）57185586718 +86-13336195806 |
China | 29792 | 60 | |
| +86-0371-55170693 +86-19937530512 |
China | 21632 | 55 | |
| 008657128800458; +8615858145714 |
China | 7738 | 55 | |
| +86-0371-86658258 +8613203830695 |
China | 29871 | 58 | |
| +86 18953170293 | China | 2930 | 58 | |
| +86-86-5926051114 +8618959220845 |
China | 6383 | 58 | |
| 86-13657291602 | CHINA | 22963 | 58 |