109581-93-3
基本信息
他克莫司,一水
他克莫司一水合物
FK-506一水合物
他克莫司 USP标准品
135175
CS-1308
Tacarolimus
[3R[E(1S,3S,4S)
tacrolimushydrate
FK-506 MONOHYDRATE
Tacrolimus (150 mg)
FR900506 monohydrate
tsukubaenolidehydrate
物理化学性质
| 熔点 | 127-129° |
| 比旋光度 | D23 -84.4° (c = 1.02 in chloroform) |
| 储存条件 | −20°C |
| 溶解度 | DMSO：可溶，20mg/mL |
| 形态 | 粉末 |
| 颜色 | 白色到近乎白色 |
| Merck | 14,9025 |
| InChIKey | NWJQLQGQZSIBAF-MLAUYUEBSA-N |
安全数据
| 危险性符号(GHS) |  GHS06 |
| 警示词 | 危险 |
| 危险性描述 | H301 |
| 防范说明 | P301+P310+P330 |
| 危险品标志 | T |
| 危险类别码 | 25 |
| 安全说明 | 45 |
| 危险品运输编号 | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS号 | KD4201200 |
| 危险等级 | 6.1 |
| 包装类别 | III |
| 海关编码 | 2934990002 |
| 毒性 | LD50 i.p. in mice: >200 mg/kg (Kino); LD50 in male, female rats (mg/kg): 57.0, 23.6 i.v.; 134, 194 orally (Ohara) |
常见问题列表
PP2B (calcineurin phosphatase)
Autophagy inducer
Tacrolimus monohydrate (FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate) inhibits calcium-dependent events, such as IL-2 gene transcription, NO synthase activation, cell degranulation, and apoptosis. Tacrolimus also potentiates the actions of glucocorticoids and progesterone by binding to FKBPs contained within the hormone receptor complex, preventing degradation. The agent may enhance expression of the TGFβ-1 gene in a fashion analogous to that demonstrated for CsA. T cell proliferation in response to ligation of the T cell receptor is inhibited by Tacrolimus. Treatment with a low concentration of Tacrolimus (FK506,10 μg/L) does not significantly affect the proliferation of MH3924A cells (P=0.135). Upon treatment with higher concentrations of Tacrolimus (100-1,000 μg/L), the proliferation of MH3924A cells is significantly enhanced (P<0.01). Treatment with AMD3100 at any concentration (10, 50 or 100 μg/L), has no obvious effect on MH3924A cell proliferation (P>0.05). However, when different concentrations of AMD3100 are combined with 100 μg/L Tacrolimus, the in vitro proliferation of MH3924A cells is increased (P<0.01).
The therapeutic effect of Tacrolimus is investigated on progression and perpetuation of colitis by administering Tacrolimus to Dextran sulfate sodium (DSS)-treated mice from Days 10 to 16 or to 23. At Days 17 and 24, colon length is significantly shortened, and colon weight is significantly higher in DSS-treated control animals than in normal animals. In addition, colon weight per unit length in the control group is more than twice that in the normal group. While both 7 and 14 d treatment with Tacrolimus significantly suppresses increases in colon weight per unit length in DSS-treated animals compared with the control group, this treatment does not actually restore the colon shortening. In addition, this inhibitory effect of Tacrolimus on increases in colon weight per unit length is more pronounced with 14-d than 7-d treatment, as shown by the inhibitory percentages (59% vs. 28%).