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他克莫司一水合物
产品纠错
CAS号:109581-93-3 | 英文名称:Tacrolimus monohydrate
分子式
分子量
EINECS号
MDL
Smiles
InChIKey
乙二醇化学百科
基本信息
中文名称 他克莫司
英文名称 Tacrolimus
CAS号 109581-93-3
分子式 C44H71NO13
分子量 822.05
EINECS号 617-559-7
物化性质
熔点 127-129°
比旋光度 D23 -84.4° (c = 1.02 in chloroform)
溶解度 DMSO:可溶,20mg/mL
形态 粉末
颜色 白色到近乎白色
Merck 14,9025
安全信息
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
海关编码 2934990002
危险等级 6.1
包装类别 III
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)
生产及用途
Tacrolimus monohydrate (FK506 monohydrate) 是大环内酯类化合物,Tacrolimus monohydrate 与 FK506 结合蛋白 (FKBP) 结合形成复合物并抑制钙调神经磷酸酶 (calcineurin phosphatase),从而抑制 T 淋巴细胞信号转导和 IL-2 转录。具有强免疫抑制特性。

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%).

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Tacrolimus Monohydrate
询价
上海阿拉丁生化科技股份有限公司
2023-10-02

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