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Tacrolimus

(Synonyms: 他克莫司; FK506; Fujimycin; FR900506)

目录号: PC61244 纯度: ≥99%

Tacrolimus (FK506)，大环内酯类，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。Tacrolimus (FK506)，大环内酯类，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。

CAS No. :104987-11-3

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PC61244-25mg	25mg	¥415.00	请登录
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中文名称	Tacrolimus
中文别名	他克莫司;大环哌喃;他克莫斯;泰克利马;他克莫司(免疫抑制药,皮炎);富吉霉素;藤毒素;夫西地酸;钾环己基三氟硼酸酯;科研实验他克莫司;临床实验他克莫司;他克莫司标准品;他克莫司大环哌喃;他克莫司植物提取物,标准品,对照品;他克莫司标准品(JP);他克莫司粉末;他克莫司固体状;他克莫司中间体;医药级他克莫司;FK506钙调磷酸酶(PP-2B)抑制剂;氧化铁红;他克莫司杂质
英文名称	Tacrolimus
英文别名	Tacrolimus;(2-propenyl)-,(3s-(3r(e(1s,3s,4s)),4s,5r,8s,9e,12r,14r,15s,16r,18s;16-dimethoxy-4,10,12,18-tetramethyl-8-3-(2-(4-hydroxy-3-methoxycyclohexyl)-1;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)-14,16-dim;6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-5;fr900506;prograf;tsukubaenolide;FK-506;C44H69NO12;FK 506;FK-506 (Tacrolimus);FK506(Tacrolimus);Tacrolimus (FK-506 , FR-900506, Fujimycin,Prograf®,Protopic®,Advagraf®);Tacrolimus solution;Tarcolimus; Fujimycin;Tacrolimus (FK506);ferric oxide;Tacrolimus Impurity;Protopic;FK506;Tacrolimus anhydrous;Modigraf;Protopy;LCP-Tacro;Anhydrous Tacrolimus;Advagraf;8-DEETHYL-8-[BUT-3-ENYL]-ASCOMYCIN;K506;Astagraf XL;Prograf (TN);Tacarolimus;FR 900506;Y5L2157C4J;FK5;Tacrolimus (anhydrous);Prograft;Tacrolimus [USAN];Graceptor;Envarsus;Avagraf;L 679934;Envarsu
Cas No.	104987-11-3
分子式	C₄₄H₆₉NO₁₂
分子量	804.02
包装储存	4°C, Keep In Dark；*In solvent : -80°C, 6 months; -20°C, 1 month (Keep In Dark)；
详情描述	Tacrolimus (FK506)，大环内酯类，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。Tacrolimus (FK506)，大环内酯类，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。

生物活性	Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties.
性状	Solid
IC50 & Target[1][2]	Macrolide

体外研究(In Vitro)

Tacrolimus (FK506) 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 effec

体内研究(In Vivo)

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. 2

运输条件

Room temperature or refrigerated transport.

储存方式

4°C, Keep In Dark；*In solvent : -80°C, 6 months; -20°C, 1 month (Keep In Dark)；

ClinicalTrial

结构分类

Antibiotics
Macro

来源

fungus Streptomyces tsukubaensis.

溶解度数据	体外研究: DMSO : ≥ 150 mg/mL(186.56 mM) *≥ means soluble, but saturation unknown. 配制储存液

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Tacrolimus

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