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Published TCIMAIL newest issue No.198
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CAS RN: 109581-93-3 | Product Number: M2258
Tacrolimus Monohydrate
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Purity: >80.0%(HPLC)
Synonyms:
- FK 506 Monohydrate
Product Documents:
| Size | Unit Price | Belgium | Japan* | Quantity |
|---|---|---|---|---|
| 10MG |
€109.00
|
1 | ≥40 |
|
| 50MG |
€383.00
|
1 | 10 |
|
*Stock available in Belgium will be delivered in 1 to 3 days
*Stock available in Japan will be delivered in 1 to 2 weeks (excludes regulated items and dry ice shipments).
| Product Number | M2258 |
Purity / Analysis Method 
|
>80.0%(HPLC) |
| Molecular Formula / Molecular Weight | C__4__4H__6__9NO__1__2·H__2O = 822.05 |
| Physical State (20 deg.C) | Solid |
| Storage Temperature
|
Frozen (<0°C) |
| Condition to Avoid | Heat Sensitive |
| CAS RN | 109581-93-3 |
| Related CAS RN
|
104987-11-3 |
| Reaxys Registry Number | 6265275 |
| PubChem Substance ID | 160871186 |
| Merck Index (14) | 9025 |
| MDL Number | MFCD11045918 |
Specifications
| Appearance | White to Almost white powder to crystal |
| Purity(HPLC) | min. 80.0 area% |
| Melting point | 125.0 to 129.0 °C |
Properties (reference)
| Melting Point | 127 °C |
| Solubility in water | Insoluble |
| Solubility (soluble in) | Acetone, Ethanol, Methanol |
GHS
| Pictogram |
|
| Signal Word | Danger |
| Hazard Statements | H301 : Toxic if swallowed. |
| Precautionary Statements | 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. |
Related Laws:
| RTECS# | KD4201200 |
Transport Information:
| UN Number | UN2811 |
| Class | 6.1 |
| Packing Group | III |
| HS Number | 2934999090 |
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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