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Такролимус
- английское имяTacrolimus
- CAS №104987-11-3
- CBNumberCB9772399
- ФормулаC44H69NO12
- мольный вес804.02
- EINECS1308068-626-2
- номер MDLMFCD00869853
- файл Mol104987-11-3.mol
Температура плавления | 113-115°C |
Температура кипения | 871.7±75.0 °C(Predicted) |
плотность | 1.19±0.1 g/cm3(Predicted) |
Fp | 2℃ |
температура хранения | Sealed in dry,Store in freezer, under -20°C |
растворимость | DMSO: >3 mg/mL |
форма | solid |
пка | 9.97±0.70(Predicted) |
цвет | white |
Растворимость в воде | Freely soluble in DMSO or ethanol. Poorly soluble in water.Soluble in dimethyl sulfoxide, ethanol, water, acetone, chloroform, ethyl acetate, ether, methanol and dimethyl formamide. |
BCS Class | 2 |
Стабильность | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months. |
ИнЧИКей | QJJXYPPXXYFBGM-LFZNUXCKSA-N |
Справочник по базе данных CAS | 104987-11-3(CAS DataBase Reference) |
Словарь онкологических терминов NCI | tacrolimus |
FDA UNII | Y5L2157C4J |
Словарь наркотиков NCI | Prograf |
Код УВД | D11AH01,L04AD02 |
Коды опасности | T,Xi,Xn,F | |||||||||
Заявления о рисках | 25-36/37/38-36-20/21/22-11 | |||||||||
Заявления о безопасности | 45-36-26-36/37-16-60-20 | |||||||||
РИДАДР | UN 2811 6.1/PG 3 | |||||||||
WGK Германия | 3 | |||||||||
RTECS | KD4201200 | |||||||||
Класс опасности | 6.1 | |||||||||
кода HS | 29349990 | |||||||||
Банк данных об опасных веществах | 104987-11-3(Hazardous Substances Data) | |||||||||
NFPA 704: |
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рисовальное письмо(GHS)
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рисовальное письмо(GHS)
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сигнальный язык
опасность
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вредная бумага
H301:Токсично при проглатывании.
H361f:Предполагается, что данное вещество может отрицательно повлиять на способность к деторождению.
H373:Может поражать органы (Нервная система) в результате многократного или продолжительного воздействия при вдыхании.
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оператор предупредительных мер
P202:Перед использованием ознакомиться с инструкциями по технике безопасности.
P260:Не вдыхать газ/ пары/ пыль/ аэрозоли/ дым/ туман.
P264:После работы тщательно вымыть кожу.
P270:При использовании продукции не курить, не пить, не принимать пищу.
P280:Использовать перчатки/ средства защиты глаз/ лица.
P301+P310:ПРИ ПРОГЛАТЫВАНИИ: Немедленно обратиться за медицинской помощью. Прополоскать рот.
Такролимус химические свойства, назначение, производство
Описание
Tacrolimus, isolated from the microorganism Streptomyces tsukubaensis, is a macrolide immunosuppressant developed by Fujisawa for organ transplantation. It displays similar but more potent immunosuppressive activity than cyclosporin. It inhibits both cell mediated and humoral immune responses. In animal models of organ transplantation, tacrolimus has been shown to prolong survival of hepatic, renal, cardiac, small intestine, pancreatic and skin allografts and to reverse cardiac and renal allograft rejection. It has been used effectively in humans as rescue or primary immunosuppressant therapy in liver or kidney transplantation. Compared to cyclosporin, tacrolimus causes reduced incidence of infectious complications and of hypertension and hypercholesterolemia for the allograft recipients. In common with cyclosporin, tacrolimus binds with high affinity to a family of cytoplasmic immunosuppressant binding proteins, the immunophilins. This tight complex is proposed as the biologically active moiety that interacts with intracellular molecules involved in signal transduction.It inhibits phosphatase activity of calcineurin, an action that may impair the generation and/or activation of nuclear transcription factors required for lymphokine (particularly interleukin-2) gene expression. Tacrolimus has also been reported to have potential in multiple sclerosis, psoriasis, rheumatoid arthritis and uveitis associated with Behcet‘s disease.Химические свойства
White Crystalline SolidИспользование
FK-506 (Tacrolimus) is a macrolide immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune systemОпределение
ChEBI: Tacrolimus is a macrolide containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.Показания
Tacrolimus is a macrolide lactone originally derived from Streptomyces tsukubaensis. Although structurally unrelated to cyclosporine, tacrolimus has a very similar mechanism of action; that is, it blocks the production of proinflammatory cytokines by T lymphocytes by inhibiting calcineurin.Tacrolimus, however, appears to be 10 to 100 times as potent as an immunosuppressive. Oral tacrolimus (FK506) is used for prevention of organ rejection in recipients of renal and hepatic transplants.Общее описание
Immunosuppressant that blocks T-cell proliferation in vitro by inhibiting the generation of several lymphokines, especially IL-2. Shown to inhibit the activity of FK-506 Binding Protein, thereby reversing its effects on sarcoplamic reticulum Ca2+ release. Shown to inhibit the Ca2+-dependent phosphatase, Calcineurin (Cat. No. 539565), as well as Na+-K+-ATPase in nephron segments. Also shown to inhibit aldosterone-induced synthesis of Giα-3 protein.Клиническое использование
A topical formulation (Protopic) has recently been approved for treatment of moderate to severe atopic dermatitis in children and adults who have not responded to other therapies. Levels of systemic absorption are low even when applied to a relatively large body surface area.Побочные эффекты
Local irritant reactions (burning, stinging, erythema) are a common side effect, but these usually resolve within the first few days of treatment. The major benefit of topical tacrolimus over topical corticosteroids is that tacrolimus does not cause atrophy, striae, or telangiectasia, even with chronic use.Такролимус запасные части и сырье
Такролимус поставщик
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