Tacrolimus (FK506)

For research use only. Not for use in humans.

目录号：S5003 别名： FR900506, Fujimycin, Prograf 中文名称：他克莫司

Tacrolimus (FK506) Chemical Structure

CAS No. 104987-11-3

Tacrolimus (FK506, FR900506, Fujimycin, Prograf) 是一种23元大环内酯物，通过结合到抑免蛋白FKBP12 (FK506 结合蛋白)产生新的复合物，从而降低T细胞中肽酰脯氨酰异构酶活性。Tacrolimus 也可抑制calcineurin钙调磷酸酶的磷酸酶活性。Tacrolimus 可诱导血管内皮细胞的自噬。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1137.06 现货
RMB 744.25 现货
RMB 3538.67 现货
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客户使用Selleck生产的Tacrolimus (FK506)发表文献52篇：

产品安全说明书

FKBP抑制剂选择性比较

生物活性

产品描述 Tacrolimus (FK506, FR900506, Fujimycin, Prograf) 是一种23元大环内酯物，通过结合到抑免蛋白FKBP12 (FK506 结合蛋白)产生新的复合物，从而降低T细胞中肽酰脯氨酰异构酶活性。Tacrolimus 也可抑制calcineurin钙调磷酸酶的磷酸酶活性。Tacrolimus 可诱导血管内皮细胞的自噬。
靶点
FKBP12 [1]
(T cells)		 calcineurin [6]
()
体外研究

FK-506和环孢霉素A阻断细胞质成分的移位，而不影响T淋巴细胞中核亚基的合成。[1] FK-506通过抑制需要白细胞介素-2转录诱导的Ca(2+)-依赖过程，阻止T细胞增殖。[2] FK 506结合于不同的细胞内蛋白质(免疫亲和素)家族，学术上称为亲环素类和FK 506结合蛋白(FKBPs)。FK-506特异性抑制细胞内磷酸酶，在药物浓度下，抑制活化的T细胞中白介素2的产生。[3] FK-506和CsA通过抑制早期钙相关的涉及淋巴因子表达，凋亡，和脱粒作用，在细胞中几乎发挥相同的生物学作用。FK-506与细胞内受体家族结合，学术上称为FK-506结合蛋白(FKBPs)。[4]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human U251 cells M2f5ZmZ2dmO2aX;uJIF{e2G7 NVu5VIxSUW6qaXLpeIlwdiCxZjDTRXAyOzBiaX6gWmVITi2|dHnteYxifGWmIHj1cYFvKFV{NUGgZ4VtdHNiYomgVGxCWCC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDJR|UxRTF|Lkigcm0> MlrrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd4NEOxNVIoRjF5NkSzNVEzRC:jPh?=
human WiDr cells MoT5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGfXcYZKdmirYnn0bY9vKG:oIGPBVFE{OCCvZXTpZZRm\CClZXzsJIdzd3e2aDDpckBpfW2jbjDXbWRzKGOnbHzzMEBKSzVyPUGwMlkhdk1? NILZbY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{[0N|EyOid-MUe2OFMyOTJ:L3G+
human T-cell M3;HW3Bzd2yrZnXyZZRqd25iYYPzZZk> MWnJckB3cXS{bzDpcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVD3j[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;MD61JI5O MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek84PTN5M{OxK|44PTN5M{OxQE9iRg>?
rat RBL2H3 cells NWXzR|dDTnWwY4Tpc44h[XO|YYm= MY[xOUBucW6| M{HJZWFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgbY4hemG2IGLCUFJJOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGRPWC2EU1GtbY5lfWOnZDDUUmYu[WyyaHGgdJJw\HWldHnvckBxemWrbnP1ZoF1\WRiZn;yJFE2KG2rboOgdJJqd3JiRF7QMWJUSSClaHHscIVv\2VibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BjgSCHTFnTRUwhUUN3ME2wMlI2KG6P NX\Sc5ZqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0NVAxQDRpPkKyOFExODh2PD;hQi=>
rat RBL2H3 cells M3nDbmZ2dmO2aX;uJIF{e2G7 MX6xOkBp MlrwTY5pcWKrdHnvckBw\iCWTl[tZYxxcGFicILv[JVkfGmxbjDpckBz[XRiUlLMNmg{KGOnbHzzJIFnfGW{IEG2JIhzeyCkeTDFUGlUSSxiSVO1NF0xNjJ3IH7N M3;ic|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{mxNFc3Lz5{M{e5NVA4PjxxYU6=
PBMCs MXnGeY5kfGmxbjDhd5NigQ>? NFrQVI1KdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUU[QLXfhcY1iKHC{b3T1Z5Rqd25iKFHueIkuS0R|IH3vco9kdG:wYXygZY51cWKxZImgd5RqdXWuYYTl[EBidmRiY4XseJVz\WRiQ1S0JJBwe2m2aY\lJINmdGy|IID1dolncWWmIH\yc40hcHWvYX6gdIVzcXCqZYLhcEBjdG:xZDDtc45wdnWlbHXhdkBk\WyuKTygTWM2OCB;IECuNFAxODZizszNMi=> M{PHSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3M{[5N|k6Lz5zNUO2PVM6QTxxYU6=
PBMCs NITJPJFHfW6ldHnvckBie3OjeR?= M3OxPGlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBKVC13IIDyc4R2[3Srb36gLGFvfGlvQ1SzJI1wdm:lbH;uZYwh[W62aXLv[Jkhe3SrbYXsZZRm\CCjbnSgZ5VtfHW{ZXSgR2Q1KHCxc3n0bZZmKGOnbHzzJJB2emmoaXXkJIZzd21iaIXtZY4heGW{aYDo[ZJidCCkbH;v[EBud26xboXjcIVieiClZXzsLUwhUUN3MDC9JFAvODByME[g{txONg>? NWrCNoVNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWzOlk{QTlpPkG1N|Y6Ozl7PD;hQi=>
T-cells MXXGeY5kfGmxbjDhd5NigQ>? MnvCWIhmKGOxbYDveY5lKHejczD0[ZN1\WRiZn;yJIl1eyCrbnjpZol1d3K7IHHjeIl3cXS7IHHnZYlve3RiVD3j[YxtKHC{b3zp[oVz[XSrb36geZNqdmdibYXybY5mKHOybHXubYMhXC2lZXzsd{whUUN3MDC9JFAvODByMjFOwG0v MmT6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB2NUC5PFcoRjFyNEWwPVg4RC:jPh?=
RBL-2H3 NWm5R2FlTnWwY4Tpc44h[XO|YYm= M{KycmlvcGmkaYTpc44hd2ZiRF7QO{1DW0FiYX70bYdmdi2rbnT1Z4VlKFSQRnHsdIhiKHKnbHXhd4UhcW5icnH0JHJDVC1{SEOgZ4VtdHNuIFnDOVAhRSByLkCwNFI2KM7:TT6= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjlyMU[5Okc,OTZ7MEG2PVY9N2F-
Jurkat T M4X2NGludXWwb4P1dJBz\XO|aY\lJIF{e2G7 MYSxOUB1dyB|MDDtbY5{ Mni5TY1ufW6xc4XwdJJme3OrdnWgZYN1cX[rdImgbY4hWE2DL3nvco9ugWOrbjDzeIlufWyjdHXkJIh2dWGwIFr1dotifCCWIHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKEmOMjDwdo9lfWO2aX;uJJBz\XS{ZXH0[YQh\m:{IEG1JJRwKDNyIH3pcpMh\m:ubH;3[YQh[nliUF3BM4lwdm:veXPpckBi\GSrdHnvckBu\WG|dYLl[EBi\nSncjCxPEB1dyB{MDDodpMh[nliRVzJV2EtKEmFNUCgQUAxNjN4IN88UU4> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDRzMkKwOEc,Ojh2MUKyNFQ9N2F-
HEK293 NVrETZU3TnWwY4Tpc44h[XO|YYm= NETHUm1VWF:WUlHOV3BQWlSHUkqgbY5pcWKrdHnvckBw\iCSaHHscI9q\GmwIIXweIFs\SBqUHjhcIxwcWSrbkqgNUB2VSliaX6gU2FVWC2FLXX4dJJme3OrbnegTGVMOjl|IHPlcIx{NCCLQ{WwJF0hOy55IN88UU4> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPDV|MEmwO{c,OTR3M{C5NFc9N2F-
Jurkat T M4nNT2FvfGmrbn\sZY1u[XSxcomgZZN{[Xl? NX7QcVRXOjBibXnudy=> MXTBcpRqNWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDpckBRVUFxaX;uc416[2mwIIP0bY12dGG2ZXSgbJVu[W5iSoXyb4F1KFRiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGlNNTJic3XjdoV1cW:wIIDy[Ylv[3WkYYTl[EBnd3JiMkCgcYlveyCob3zsc5dm\CCkeTDQUWEwcW:wb335Z4lvKHO2aX31cIF1cW:wIH3lZZN2emWmIHHmeIVzKDF{IHjyd{BjgSCHTFnTRUwhUUN3MDC9JFUvQCEQvF2u NH\o[FI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEWwPVU2Oid-Mki1NFk2PTJ:L3G+

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
GluA1 / pGluA1(S845) / GluA2 / GluA3 / Calcineurin; 

PubMed: 26455952     


Representative immunoblots and quantitative analysis of synaptosomes from cultured mutant hippocampal neurons in the presence and absence of FK506 treatment showing a selective increase in total GluA1 and GluA1 S845 phosphorylation [pGluA1(S845)] (n=10 experiments, *p<0.05 and ***p<0.001, unpaired two-tailed student's t-test). 

p-JNK / JNK / p-ERK / ERK / Cytochrome c / cleaved caspase-3; 

PubMed: 23470533     


Effect of FK506 on protein expressions of p-JNK, p-ERK, cytosolic cytochrome c and cleaved caspase-3. Cells were incubated either in the absence of (control) or in the presence of FK506 (12.5, 25 and 50 μM) for 8 h, and protein expressions of p-JNK, p-ERK, cytosolic cytochrome c and cleaved caspase-3 were determined using western blotting. Increasing expressions of p-JNK, p-ERK, cytosolic cytochrome c and cleaved caspase-3 were observed in fibroblasts after FK506 treatment at increasing concentrations, and peaked at the concentration of 50 μM.

p-S6K(S371) / S6K / p-Erα(S167) / Erα; 

PubMed: 29344249     


MCF-7 cells were incubated with PS, OA (100 nM), Cal A (1 nM), FK506 (10 nM), or DMSO (0.1%, vehicle) in E2 (10 nM) medium. Phosphorylation was determined by western blotting. 

26455952 23470533 29344249
Immunofluorescence
FKBP52 / p23 / hsp90; 

PubMed: 20796173     


Subcellular localization of FKBP52, hsp90 and p23 in N2a cells. (a) Images by confocal microscopy of undifferentiated cells prior (0 h) or after (3 h and 24 h) of treatment with FK506. Image on the right hand shows a wider field.

FKBP51; 

PubMed: 20796173     


FKBP51 concentrates in transcriptionally active nuclear domains. Cells were treated with FK506 for 6 h and pre-mRNAs were labeled with Br-UTP. Bars= 10 μm

Tom20 / JC-1 / ROS / NF-κB; 

PubMed: 30294901     


TH2849 protects mitochondrial from damage induced by MPP+. Representative confocal image of MDA‐MB‐231 cells incubated with treated with 1‰ DMSO, 10 μmol/L MPP+ alone, or co‐treated with 1 μmol/L rapamycin, 10 μmol/L FK506, 1 μmol/L TH 2451, and 1 μmol/L TH 2849 for 24 h, and then, the immunofluorescence experiment was performed with the primary antibody against (A) Tom20 and (D) NF‐Κb, or the fluorogenic probe DCFH‑DA was used to detect the ROS levels (C). B, EGFP‐LC3 transfected PC12 cells were treated with 10 μmol/L MPP+ alone or co‐treated with 1‰ DMSO, 1 μmol/L rapamycin, 10 μmol/L FK506, 1 μmol/L TH 2451, and 1 μmol/L TH 2849 for 24 h. Mitochondrial transmembrane potential (ΔΨm) was detected by JC‐1. All the substances were dissolved in DMSO. Scale bars: 10 μm. n = 3

20796173 30294901
Growth inhibition assay
Cell viability; 

PubMed: 23470533     


Effect of FK506 on fibroblast proliferation in vitro. Rat skin fibroblasts were treated with increasing concentrations of FK506 for 8 h. The viable cells were measured by CCK-8 assay. FK506 inhibited fibroblast proliferation in a dose-dependent manner. Cell viability reached a relatively minimal level at 75 μM. *P<0.05, **P<0.01 compared with control. All experiments were preformed three times with comparable results

23470533
体内研究

大鼠行为疼痛评估中，FK-506导致痛觉过敏和异常疼痛刺激下爪子和尾巴收缩的阈值增加。在大鼠体内，FK-506也会导致血清硝酸盐和硫代巴比妥酸活性产物(TBARS)水平降低，并伴随组织髓过氧化物酶(MPO)和总钙水平降低，然而，会升高组织中还原型谷胱甘肽的水平。在缺血再灌注损伤(I/R)的大鼠体内，FK-506可以改善加重的神经水肿和轴突变性。[5]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 94 mg/mL (116.91 mM)
Ethanol 83 mg/mL (103.23 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)：
5% DMSO+corn oil
 15mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 804.02
化学式

C44H69NO12
CAS号 104987-11-3
储存条件 粉状
溶于溶剂
别名 FR900506, Fujimycin, Prograf

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04505878 Not yet recruiting Drug: Vitamin C Primary Graft Dysfunction|Lung Transplant; Complications University of Wisconsin Madison April 2021 Phase 2
NCT04646603 Not yet recruiting Drug: MRG-001|Drug: Placebo COVID-19 MedRegen LLC|Kendall Healthcare Group Ltd. January 5 2021 Phase 1|Phase 2
NCT04645667 Not yet recruiting Drug: Tacrolimus Acute GVHD UNC Lineberger Comprehensive Cancer Center|University of North Carolina Chapel Hill December 1 2020 --
NCT04530630 Recruiting Drug: BIKTARVY 50Mg-200Mg-25Mg Tablet HIV Infections|Renal Transplant Rejection Weill Medical College of Cornell University|Gilead Sciences November 9 2020 Phase 4
NCT04587024 Recruiting Other: mHealth intervention|Other: standard of care Medication Adherence|Liver Transplantation|Kidney Transplantation Johns Hopkins University November 20 2020 Not Applicable

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操作手册

如果有其他问题，请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1：

    we would like to inject it subcutaneously into rats, Can we mix the FK506 with 5% dextrose to a concentration of 5mg/ml to prepare the solution?

  • 回答：

    You can dissolve FK506 with DMSO to prepare the stock solution, and then dilute by 5% dextrose. However, we don't have the information about the solubility in this condiation. Or you can use the vehicle we tested: 30% PEG400/0.5% Tween80/5% propylene glycol (Solubility: 30mg/ml).

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID