Tacrolimus (FK506)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Tacrolimus(FK506)是一种有效的和选择性的T淋巴细胞抑制剂和大环内酯类免疫抑制剂[1]。
在体外,tacrolimus(FK506)抑制白细胞介素2(IL-2)的产生和混合淋巴细胞培养物的反应。此外,tacrolimus(FK506)加入细胞培养物可抑制小鼠或人混合淋巴细胞的反应性和细胞毒性T细胞的产生。而且,tacrolimus(FK506)剂量依赖地抑制不同刺激诱导的各种细胞因子的产生,包括IL-2、IL-3、IL-4和γ干扰素。在动物移植模型中,tacrolimus有效阻止移植排斥反应。在实验性肝移植中,tacrolimus显著有效,并具有嗜肝性[1]。
参考文献:
[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.
- 1. PENGYU JIA, NAN WU, et al. "Different roles of BAG3 in cardiac physiological hypertrophy and pathological remodeling." Transl Res. 2021 Jul;233:47-61. PMID:33578031
- 2. Carsten Deppermann, Moritz Peiseler, et al. "Tacrolimus impairs Kupffer cell capacity to control bacteremia: why transplant recipients are susceptible to infection." Hepatology. 2020 Aug 6. PMID:32761929
- 3. Souvik Dey, Alaa Eisa, et al. "Roles of glycogen synthase kinase 3 alpha and calcineurin in regulating the ability of sperm to fertilize eggs." FASEB J. 2020;34(1):1247–1269. PMID:31914663
- 4. 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
- 5. 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
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 804.02 |
Cas No. | 104987-11-3 |
Formula | C44H69NO12 |
Solubility | ≥26.6 mg/mL in DMSO; insoluble in H2O; ≥84.5 mg/mL in EtOH |
SDF | Download SDF |
Canonical SMILES | CO[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 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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 |
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 |
质量控制和MSDS
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