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CAS RN: 109581-93-3 | 產品號碼: M2258
Tacrolimus Monohydrate
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產品規格
| Appearance | White to Almost white powder to crystal |
| Purity(HPLC) | min. 80.0 area% |
| Melting point | 125.0 to 129.0 °C |
性質
| 熔點 | 127 °C |
| 水溶性 | Insoluble |
| 溶解性（可溶於） | Acetone, Methanol, Ethanol |
GHS
| 圖形表示 |
|
| 信號詞 | Danger |
| 危險性說明 | H301 : Toxic if swallowed. |
| 防範說明 | P501 : Dispose of contents/ container to an approved waste disposal plant. P270 : Do not eat, drink or smoke when using this product. P264 : Wash skin thoroughly after handling. P301 + P310 + P330 : IF SWALLOWED: Immediately call a POISON CENTER/doctor. Rinse mouth. P405 : Store locked up. |
相關法規
| RTECS # | KD4201200 |
運輸資料
| UN編號 | UN2811 |
| 類別 | 6.1 |
| 包裝類別 | III |
| HS編碼* | 2934.99-000 |
Application
Bone research
Reference
- In Vitro Bone Formation Induced by Immunosuppressive Agent Tacrolimus Hydrate (FK506)
Application
Tacrolimus: A Calcineurin Inhibitor with Immunosuppressive Properties
Tacrolimus, known as FK506, is a macrolide immunosuppressant produced by Streptomyces tsukubaensis. Tacrolimus is practically insoluble in water, freely soluble in ethanol and DMF, and very soluble in methanol and chloroform. Tacrolimus inhibits T-lymphocyte activation, although the exact mechanism of action is not known. Experimental evidence suggests that tacrolimus is inactive by itself and requires binding to an intracellular protein, FK506 binding protein-12 (FKBP-12), for activation in cells. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin (a calcium and calmodulin dependent protein phosphatase) is then formed and the phosphatase activity of calcineurin inhibited. This effect may prevent both T-lymphocyte signal transduction and IL-2 transcription. Cyclosporin A [C2408] also inhibits calcineurin but is less potent than tacrolimus. Tacrolimus is mainly metabolized by cytochrome P 450 IIIA (CYP3A) subfamilies. (The product is for research purpose only.)
References
- Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes
- The mechanism of action of cyclosporin A and FK506
- Crystal structures of human calcineurin and the human FKBP12-FK506-calcineurin complex
- Drug target validation and identification of secondary drug target effects using DNA microarrays
- FK506, an immunosuppressant targeting calcineurin function (a review)
- Effects of FK506 and other immunosuppressive anti-rheumatic agents on T cell activation mediated IL-6 and IgM production in vitro
- Mechanisms of clinically relevant drug interactions associated with tacrolimus (a review)
PubMed Literature
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