他克莫司一水合物 CAS#: 109581-93-3

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他克莫司一水合物

生物活性靶点体外研究体内研究 用途与合成方法 MSDS 他克莫司一水合物价格(试剂级) 上下游产品信息

中文名称	他克莫司一水合物
中文同义词	他克莫司一水合物;FK-506一水合物;他克莫司,一水;他克莫司水合物;他克莫司 USP标准品;(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26AS)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26A-十六氢-5,19-二羟基-3-[(1E)-2-[(1R,3R,4R)-4-羟基-3-甲氧基环己基]-1-甲基乙烯基]-14,16-二甲氧基-4,10,12,18-四甲基-8-(2-丙烯基-1-基)-15,19-环氧-3H-吡啶并[2,1-C][1,4]氧杂氮杂环二十三烯-1,7,20,21(4H,23H)-四酮一水合物;他克莫司对照品带水;他克莫司一水物
英文名称	Tacrolimus Monohydrate
英文同义词	FK-506;15,19-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, 5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propenyl)-, monohydrate, [3S-[3R*[E(1S*,3S*,4S*)],4S*,5R*,8S*,9E,12R*,14R*,15S*,16R*,18S*,19S*,26aR*]]-;TACROLIMUS HYDRATE/TSUKUBAENOLIDE HYDRATE;(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-Hexadecahydro-5,19-dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propen-1-yl)-15,19-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)tetrone;Tacrolimus (150 mg);(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-Hexadecahydro-5,19-dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-Methoxycyclohexyl]-1-Methylethenyl]-14,16-diMethoxy-4,10,12,18-tetraMethyl-8-(2-propen-1-yl)-;Tacrolimus monohydrate;FK-506 monohydrate, >=98%
CAS号	109581-93-3
分子式	C44H71NO13
分子量	822.05
EINECS号	617-559-7
相关类别	他克莫司杂质;医用原料;发酵类;医药原料;化学连接;原料药;抗生素;医用原料;化学试剂;化工原料;原料;精细化工原料;Signalling
Mol文件	109581-93-3.mol
结构式

他克莫司一水合物 性质

他克莫司一水合物 用途与合成方法

生物活性

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。

靶点

PP2B (calcineurin phosphatase)  
 Autophagy inducer

体外研究

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).

体内研究

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%).

安全信息

MSDS信息

他克莫司一水合物 价格(试剂级)

他克莫司一水合物 上下游产品信息