MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Tacrolimus monohydrate

CAS No. : 109581-93-3

MCE 站：Tacrolimus monohydrate

产品活性：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。

研究领域：Metabolic Enzyme/Protease  |  Autophagy  |  Apoptosis  |  Immunology/Inflammation  |  Anti-infection

作用靶点：Phosphatase  |  FKBP  |  Autophagy  |  Bacterial  |  Antibiotic

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 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).

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. 28%).

相关产品：Natural Product Library Plus  |  Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Anti-Infection Compound Library  |  Apoptosis Compound Library  |  Immunology/Inflammation Compound Library  |  Metabolism/Protease Compound Library  |  Natural Product Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Peptidomimetic Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Macrocyclic Compound Library  |  Antibacterial Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Antibiotics Library  |  Drug-Induced Liver Injury (DILI) Compound Library  |  Phosphatase Inhibitor Library  |  Rapamycin  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Puromycin dihydrochloride  |  Cycloheximide  |  Chloroquine  |  Staurosporine  |  Dexamethasone  |  Doxycycline (hyclate)  |  Actinomycin D  |  Cyclosporin A  |  G-418 disulfate  |  5-Azacytidine  |  Etoposide  |  Mitomycin C  |  CCCP  |  Nigericin sodium salt  |  Brefeldin A  |  Wortmannin  |  Everolimus  |  Resveratrol  |  Tunicamycin  |  Bleomycin sulfate  |  Hygromycin B  |  Tacrolimus  |  Ionomycin  |  Vancomycin hydrochloride  |  Streptozocin  |  Tanespimycin

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。