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Tacrolimus (FK506)

现货
Catalog No.
B2143
大环内酯类钙调神经磷酸酶抑制剂,免疫抑制剂。
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
50mg
¥ 650.00
现货
100mg
¥ 1,200.00
现货
200mg
¥ 1,800.00
现货
500mg
¥ 3,100.00
现货
1g
¥ 4,800.00
现货

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Background

Tacrolimus (FK506) is a potent and selective inhibitor of T-lymphocyte and the macrolide immunosuppressant [1].

In vitro, Tacrolimus (FK506) has been reported to inhibit the interleukin 2(IL-2) production and the response of mixed lymphocyte culture. In addition, Tacrolimus (FK506) added to the cell cultures has been revealed to inhibit murine or human mixed lymphocyte reactivity and the generation of cytotoxic T cells. Furermor, Tacrolimus (FK506) has also been reported to dose-dependently suppress the production of various cytokines including IL-2, IL-3, IL-4, and γ-interferon, in response to different stimulis. Besides, Tacrolimus has shown its efficacy in the prevention of allograft rejection in animal transplant models. Tacrolimus has been found to be significantly efficient in experimental hepatic allografts, and has hepatotrophic properties [1].

References:
[1] Wallemacq PE1, Reding R. FK506 (tacrolimus), a novel immunosuppressant in organ transplantation: clinical, biomedical, and analytical aspects. Clin Chem. 1993 Nov; 39(11 Pt 1):2219-28.

文献引用

1. Peiffer BJ, Qi L, et al. "Activation of BMP Signaling by FKBP12 Ligands Synergizes with Inhibition of CXCR4 to Accelerate Wound Healing." Cell Chem Biol. 2019 May 16;26(5):652-661.e4. PMID:30827938
2. Wang Z, Wang Y, et al. "Transient receptor potential channel 1/4 reduces subarachnoid hemorrhage-induced early brain injury in rats via calcineurin-mediated NMDAR and NFAT dephosphorylation." Sci Rep. 2016 Sep 19;6:33577. PMID:27641617

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt804.02
Cas No.104987-11-3
FormulaC44H69NO12
Solubility≥26.6mg/mL in DMSO, ≥84.5 mg/mL in EtOH, <4.05 mg/mL in H2O
SDFDownload SDF
Canonical SMILESCO[C@@H]1C[C@H](/C=C(C)/[C@@H](OC([C@]2([H])CCCCN2C(C([C@]3(O)O[C@H]([C@@H](OC)C[C@H](C/C(C)=C/4)C)[C@@H](OC)C[C@H]3C)=O)=O)=O)[C@H](C)[C@H](CC([C@@H]4CC=C)=O)O)CC[C@H]1O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验:

细胞系

肝切片,人肺成纤维细胞

溶解方法

该化合物在DMSO中的溶解度 > 10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应时间

2μM和4μM、处理3天

应用

FK506在体外培养的肝切片中减少I型胶原合成 [1]。此外,FK506(2μM)减少I型胶原蛋白合成,而不影响胶原mRNA的表达 [2]。

动物实验:

动物模型

大鼠模型

剂量

4 mg/kg、腹腔注射,每日给药,持续4周;或1、2和3mg/kg、口服、连续10天

应用

FK506(4mg / kg)通过靶向大鼠中LARP6依赖性的胶原合成机制来阻止乙醇诱导的肝纤维化的早期阶段 [1]。此外,FK506(2和3mg / kg)治疗导致动脉缺血再灌注(I / R)诱导的大鼠轴突变性和组织病理学改变的减弱 [2]。

注意事项

请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

1Manojlovic, Z., Blackmon, J. and Stefanovic, B. (2013) Tacrolimus (FK506) prevents early stages of ethanol induced hepatic fibrosis by targeting LARP6 dependent mechanism of collagen synthesis. PLoS One. 8, e65897

2Muthuraman, A. and Sood, S. (2010) Pharmacological evaluation of tacrolimus (FK-506) on ischemia reperfusion induced vasculatic neuropathic pain in rats. J Brachial Plex Peripher Nerve Inj. 5, 13

生物活性

描述 FK-506,23元大环内酯,是肽基脯氨酰异构酶的抑制剂。
靶点 peptidyl-prolyl isomerase          
IC50            

质量控制

化学结构

Tacrolimus (FK506)

相关生物数据

Tacrolimus (FK506)

相关生物数据

Tacrolimus (FK506)