Tacrolimus , Analysis of standard products, ≥98% , 104987-11-3
Synonym(s):
FK-506 monohydrate;FK-506, Streptomyces sp. - CAS 104987-11-3 - Calbiochem;Tacrolimus
CAS NO.：104987-11-3
Empirical Formula: C44 H69 N O12
Molecular Weight: 804.02
MDL number: MFCD00869853
EINECS: 1308068-626-2
| Pack Size | Price | Stock | Quantity |
| 10MG | RMB221.60 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| Melting point: | 113-115°C |
| Boiling point: | 871.7±75.0 °C(Predicted) |
| Density | 1.19±0.1 g/cm3(Predicted) |
| Flash point: | 2℃ |
| storage temp. | Sealed in dry,Store in freezer, under -20°C |
| solubility | DMSO: >3 mg/mL |
| form | solid |
| pka | 9.97±0.70(Predicted) |
| color | white |
| optical activity | +62.223 (CHCl3) |
| Water Solubility | 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 |
| Stability: | 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. |
| InChIKey | QJJXYPPXXYFBGM-LFZNUXCKSA-N |
Description and Uses
FK-506 is a potent immunosuppressant in the same molecular class as cyclosporin A and rapamycin . Its mechanism of action involves the formation of a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex then inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T cell activation. The physiological effects of FK-506 also include regulation of nitric oxide neurotoxicity, neurotransmitter release, and regulation of Ca2+ release via the ryanodine and inositol-(1,4,5)-trisphosphate (IP3) receptors. In the latter case, FKBP12 forms a tight complex with both ryanodine and IP3 receptors which can be disrupted by FK-506, thereby rendering the receptors leaky to Ca2+.
Tacrolimus (fujimycin) was discovered as a potent inhibitor of IL2 production in a targeted search for novel immunosuppressants. Tacrolimus acts by blocking T cell proliferation in vitro by inhibiting the generation of several lymphokines, notably the original target IL-2. Tacrolimus inhibits the activity of FK-506 binding protein, Ca2+-dependent phosphatase and calcineurin, and activates NF-κB through phosphorylation and degradation of IκBα.
Safety
| Symbol(GHS) |   GHS06,GHS08 |
| Signal word | Danger |
| Hazard statements | H301-H361f-H373 |
| Precautionary statements | P202-P260-P264-P270-P280-P301+P310 |
| Hazard Codes | T,Xi,Xn,F |
| Risk Statements | 25-36/37/38-36-20/21/22-11 |
| Safety Statements | 45-36-26-36/37-16-60-20 |
| RIDADR | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS | KD4201200 |
| HazardClass | 6.1 |
| HS Code | 29349990 |
