Tacrolimus monohydrate|109581-93-3|(他克莫司一水合物; FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate)-陌孚医药/Medlife

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Tacrolimus monohydrate (Synonyms: 他克莫司一水合物; FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate)

目录号: PC61284 纯度: 10mM*1mL in DMSO

CAS No. :109581-93-3

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中文名称	Tacrolimus monohydrate
中文别名	他克莫司一水合物;3-甲基噻吩-2-甲基胺;Tacrolimus Monohydrate 他克莫司一水合物;他克莫司;他克莫司 USP标准品;他克莫司水合物;FK-506一水合物;大环哌喃;他克莫斯;泰克利马
英文名称	Tacrolimus monohydrate
英文别名	Tacrolimus monohydrate;TACROLIMUS;FK-506 monohydrate;C44H71NO13;FK 506;FK-506;Tacrolimus hydrate;TacroliMus(FK-506);FK 506 Monohydrate;FK-506 monohydrate,Tacrolimus;FR900506 monohydrate;Fujimycin monohydrate;Prograf;Protopic;Fujimycin;Tsukubaenolide;FK506;Tacrolimus anhydrous;Modigraf;Protopy;LCP-Tacro;Anhydrous Tacrolimus;tacrolimus (fk506);Advagraf;8-DEETHYL-8-[BUT-3-ENYL]-ASCOMYCIN;K506;Astagraf XL;Prograf (TN);FR900506;Tacarolimus;FR 900506;Y5L2157C4J;FK5;Tacrolimus (anhydrous);Prograft;Tacrolimus [USAN];Graceptor;Envarsus;Avagraf;L 679934;Envarsu;Tsukubaenolide hydrate;Tacrolimus (monohydrate);WM0HAQ4WNM
Cas No.	109581-93-3
分子式	C₄₄H₇₁NO₁₃
分子量	822.03
包装储存	4°C, Keep In Dark；*In solvent : -80°C, 6 months; -20°C, 1 month (Keep In Dark)；

生物活性	Tacrolimus monohydrate (FK506 monohydrate), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex and 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 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 AM

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

Streptomyces tsukubaensis

溶解度数据	体外研究: DMSO : 100 mg/mL(121.65 mM;Need ultrasonic) H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) 配制储存液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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