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Tacrolimus

产品编号 T2144 CAS 104987-11-3

别名: 他克莫司, Fujimycin, FK506, FR900506

Tacrolimus (Fujimycin) 可与 FKBP12 结合形成高亲和力复合物 (Ki: 0.2 nM)，抑制钙/钙调蛋白依赖性蛋白磷酸酶的活性。

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Tacrolimus, CAS 104987-11-3

规格	价格/CNY	货期
10 mg	￥ 263	现货
25 mg	￥ 423	现货
50 mg	￥ 587	现货
100 mg	￥ 936	现货
200 mg	￥ 1,470	现货
500 mg	￥ 2,670	现货
1 mL * 10 mM (in DMSO)	￥ 391	现货

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其他形式的 Tacrolimus:

Tacrolimus monohydrate
现货

选择批次

纯度: 99.94%

纯度: 99.87%

纯度: 98.98%

纯度: 98.26%

纯度: 98%

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天然产物信息

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

植物来源	天然产物 > 其他（植物来源） > 其他

产品描述	Tacrolimus (Fujimycin) can bind FKBP12 to form a high-affinity complex (Ki: 0.2 nM) which inhibits the activity of the calcium/calmodulin-dependent protein phosphatase.
靶点活性	FKBP12:0.2 nM (Kd)
体外活性	FKBP12 was first isolated from the cytosol of Jurkat T cells, as an abundant, high-affinity receptor for Tacrolimus (FK506; Kd: 0.2 nM) [1]. FK506 (100?1,000 μg/l) significantly promoted the proliferation of MH3924A cells. The invasiveness of MH3924A cells was significantly enhanced following treatment with FK506 [2]. FK506 specifically inhibits cellular calcineurin at drug concentrations that inhibit interleukin 2 productions in activated T cells [3].
体内活性	The liver of rats of the normal saline (NS) group was large, with an average weight at 15.56±11.17 g, and the liver of rats of the FK506 group was oversize, with an average weight at 28.19±3.89 g. The rate of lymph node metastasis, as well as the number of pulmonary nodules, were significantly increased in the FK506 compared to the NS group [2]. Behavioral pain assessment revealed an increase in the paw and tail withdrawal threshold in tacrolimus-treated groups against hyperalgesic and allodynic stimuli as compared to the sham control group [4].
细胞实验	Tumor cell proliferation was determined by the MTT. Briefly, after MH3924A cells had reached the logarithmic growth phase, a 0.2-ml cell suspension at 1×10^4 cells/ml was added into each well of a 96-well plate and cultured in DMEM with 10% FBS, 10 μg/l vascular endothelial growth factor and 0.1 g/l heparin for 24 h. When adherent growth was established, different concentrations of FK506 (10, 100 and 1,000 μg/l), AMD3100 (10, 50 and 100 μg/l) and FK506 (0 and 100 μg/l) + AMD3100 (0, 10, 50 and 100 μg/l) were added into the plates. Untreated cells cultured in medium alone were used as controls. After culturing for 48 h, 10 μl MTT (5 g/l) was added, and each well was incubated for 6 h; next, 150 μl/well dimethyl sulfoxide was added, followed by measurements of the absorbance at 570 mm on a spectrophotometer reader. Each well was measured three times, and each sample was assayed in triplicate [2].
动物实验	Experiments were performed in 16 healthy August Copenhagen Irish rats (male, 16–20 weeks, weighing 240–300 g). The rat model of liver tumor was established as follows: First, MH3924A cells were collected and injected into the alar skin of rats. The tumors were removed from alar skin when grown to 2×1×1 mm3, and intrahepatic tumor implantation of rats was performed under aseptic conditions as described previously (25,26). Five days later, rats were randomly divided into two groups: one group was subcutaneously injected with normal saline for 14 days (NS group, n=8, 3 mg/kg/day), and the second group was subcutaneously injected with FK506 for 14 days (FK506 group, n=8, 0.3 mg/kg/day). Forty days following implantation, rats were sacrificed, and the weight of tumor, the volume of the fluid in the ascites, the incidence of lymphatic metastasis in the abdominal cavity and of abdominal wall metastasis were measured. In addition, the lungs were irrigated with 15% Indian ink, followed by counting of the number of metastatic nodules in the lung. The tumor and adjacent tissues, as well as healthy liver tissues, were harvested and preserved in 4% formalin for later use [2].

别名	他克莫司, Fujimycin, FK506, FR900506
分子量	804.02
分子式	C44H69NO12
CAS No.	104987-11-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 80.4 mg/mL (100 mM)

DMSO: 80.4 mg/mL (100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	1.2438 mL	6.2188 mL	12.4375 mL	31.0938 mL
	5 mM	0.2488 mL	1.2438 mL	2.4875 mL	6.2188 mL
	10 mM	0.1244 mL	0.6219 mL	1.2438 mL	3.1094 mL
	20 mM	0.0622 mL	0.3109 mL	0.6219 mL	1.5547 mL
	50 mM	0.0249 mL	0.1244 mL	0.2488 mL	0.6219 mL
	100 mM	0.0124 mL	0.0622 mL	0.1244 mL	0.3109 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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浓度 (终)

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参考文献

1. Dumont FJ. FK506, an immunosuppressant targeting calcineurin function. Curr Med Chem. 2000 Jul;7(7):731-48. 2. Zhu H, et al. Tacrolimus promotes hepatocellular carcinoma and enhances CXCR4/SDF‑1α expression in vivo. Mol Med Rep. 2014 Aug;10(2):585-92. 3. Fruman DA, et al. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A. Proc Natl Acad Sci U S A. 1992 May 1;89(9):3686-90. 4. Muthuraman A, Sood S. Pharmacological evaluation of tacrolimus (FK-506) on ischemia reperfusion induced vasculatic neuropathic pain in rats. J Brachial Plex Peripher Nerve Inj. 2010 Jun 7;5:13. 6. Yuwei He, et al. Drug targeting through platelet membrane-coated nanoparticles for the treatment of rheumatoid arthritis. Nano Res. 30 June 2018. 7. Wang W, Ren S, Lu Y, et al. Inhibition of Syk promotes chemical reprogramming of fibroblasts via metabolic rewiring and H2S production. The EMBO Journal. 2021: e106771.

文献引用

1. Wang W, Ren S, Lu Y, et al. Inhibition of Syk promotes chemical reprogramming of fibroblasts via metabolic rewiring and H2S production. The EMBO Journal. 2021 Jun 1;40(11):e106771. doi: 10.15252/embj.2020106771. Epub 2021 Apr 28. 2. Chang Z, Zhang Q, Hu Q, et al. Tannins in Terminalia bellirica inhibits hepatocellular carcinoma growth via re-educating tumor-associated macrophages and restoring CD8+ T cell function. Biomedicine & Pharmacotherapy. 2022, 154: 113543. 3. Huang, Jing, et al. Osteopontin isoform c promotes the survival of cisplatin-treated NSCLC cells involving NFATc2-mediated suppression on calcium-induced ROS levels.. BMC cancer. 21.1 (2021): 1-14.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Tacrolimus 104987-11-3 Autophagy Metabolism Microbiology/Virology Others PI3K/Akt/mTOR signaling Phosphatase Antibacterial Antibiotic mTOR 他克莫司 FKBP FK506-binding protein Inhibitor Fujimycin Bacterial FR-900506 FK 506 FK506 FK-506 inhibit FR 900506 FR900506 inhibitor

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Tacrolimus

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

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剂量换算

体内实验配液计算器

技术支持

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