Tacrolimus (FK506)

目录号:S5003 别名: FR900506

Tacrolimus (FK506) Chemical Structure

Molecular Weight(MW): 804.02

Tacrolimus (FK506) 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。

规格 价格 库存 购买数量  
RMB 1137.06 现货
RMB 744.25 现货
RMB 1395.37 现货
RMB 3538.67 现货
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客户使用该产品的7个实验数据:

  • Effect of FK506 on cytosolic calcium homeostasis induced by TG and thrombin in human platelets. (A-B) Human platelets were suspended in a Ca 2+-free medium (100 µM of EGTA was added as indicated by arrowhead), and preincubated for 5 min at 37oC in the absence (solid black traces) or presence of increased concentrations (0.01-100 µM) of FK506 (light-doted and dark solid-grey traces, respectively). Cells were then stimulated with TG (200 nM; A) or Thr (0.1 U/mL; B) and 3 min later 300 μM of CaCl2 was added to extracellular medium to visualize calcium entry.

    Biochim Biophys Acta 2013 1833(3), 652-62. Tacrolimus (FK506) purchased from Selleck.

    FK506 reduces NCCE(Non-capacitative calcium entry) independently of its inhibitory effect in CaN activity. Fura-2-loaded human platelets were suspended in HBS medium containing 300 μM Ca2+ and preincubated for 5 min with increasing concentration of FK506 (0.5-50 μM), after which OAG (100 μM) was added to initiate NCCE.

    Biochim Biophys Acta, 2015, 1853(10 Pt A):2684-96.. Tacrolimus (FK506) purchased from Selleck.

  • FK506 production of S. tsukubaensis L19 and its recombinant pression of fkbN in S. tsukubaensis L19); L22, S. tsukubaensis L22 (overexpression of tcs7 in S. tsukubaensis L19); L23, S. tsukubaensis L23 (overexpression of fkbN and tcs7 in S. tsukubaensis L19).

    J Ind Microbiol Biotechnol, 2016, 43(12):1693-1703.. Tacrolimus (FK506) purchased from Selleck.

    Release of immune mediators after Tacrolimus application. Tacrolimus was applied to IL-1β/TNFα pretreated (diamonds) or unprimed (squares) Caco-2 monolayer in the indicated concentrations. Caco-2 cells in transwell inserts were transferred to culture vessels filled with heparinized whole blood of three different healthy donors (indicated by their ID-numbers). After 1 h the whole blood in the lower compartment was stimulated by LPS/SEB/anti-CD28 injection. After 6 h the Caco-2 cells were removed and the whole blood was further incubated for 18 h. Immune mediators were quantified in plasma. Depicted are stimulation indices of single experiments. I IL-17A, J TARC, K IL-13, L IL-1ra, M IL-5, N IL-10.

    2013 Natural and Medical Sciences Institute. Tacrolimus (FK506) purchased from Selleck.

  • Release of immune mediators after Tacrolimus application. Tacrolimus was applied to IL-1β/TNFα pretreated (diamonds) or unprimed (squares) Caco-2 monolayer in the indicated concentrations. Caco-2 cells in transwell inserts were transferred to culture vessels filled with heparinized whole blood of three different healthy donors (indicated by their ID-numbers). After 1 h the whole blood in the lower compartment was stimulated by LPS/SEB/anti-CD28 injection. After 6 h the Caco-2 cells were removed and the whole blood was further incubated for 18 h. Immune mediators were quantified in plasma. Depicted are stimulation indices of single experiments. A IL-1β, B IL-6, C IFNγ, D MCP-1

    2013 Natural and Medical Sciences Institute. Tacrolimus (FK506) purchased from Selleck.

    Release of immune mediators after Tacrolimus application. Tacrolimus was applied to IL-1β/TNFα pretreated (diamonds) or unprimed (squares) Caco-2 monolayer in the indicated concentrations. Caco-2 cells in transwell inserts were transferred to culture vessels filled with heparinized whole blood of three different healthy donors (indicated by their ID-numbers). After 1 h the whole blood in the lower compartment was stimulated by LPS/SEB/anti-CD28 injection. After 6 h the Caco-2 cells were removed and the whole blood was further incubated for 18 h. Immune mediators were quantified in plasma. Depicted are stimulation indices of single experiments. E IL-8, F IP-10, G TNFα, H IL-4

    2013 Natural and Medical Sciences Institute. Tacrolimus (FK506) purchased from Selleck.

  • JCI Insight, 2016, 1(10):e86331.. Tacrolimus (FK506) purchased from Selleck.

产品安全说明书

mTOR抑制剂选择性比较

生物活性

产品描述 Tacrolimus (FK506) 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。
靶点
FKBP12 [1]
(T cells)
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
rat RBL2H3 cells M362OWZ2dmO2aX;uJIF{e2G7 NWSyWGtUOTZiaB?= NGjiS2dKdmirYnn0bY9vKG:oIGTOSk1idHCqYTDwdo9lfWO2aX;uJIlvKHKjdDDSRmwzUDNiY3XscJMh[W[2ZYKgNVYhcHK|IHL5JGVNUVODLDDJR|UxRTBwMkWgcm0> MmDhNlM4QTFyN{[=
rat RBL2H3 cells NYTD[o0zTnWwY4Tpc44h[XO|YYm= M1;mb|E2KG2rboO= NVqzN3BPSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiC{YYSgVmJNOkh|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTE6SLVLTRU1qdmS3Y3XkJHRPTi2jbIDoZUBxem:mdXP0bY9vKHC{ZXnuZ5Vj[XSnZDDmc5IhOTVibXnud{BxemmxcjDEUnAuSlODIHPoZYxt\W6pZTDt[YF{fXKnZDDh[pRmeiB|MDDtbY5{KGK7IFXMTXNCNCCLQ{WwQVAvOjVibl2= MY[yNlQyODB6NB?=
human T-cell Ml\hVJJwdGmoZYLheIlwdiCjc4PhfS=> NX3oSIdJUW5idnn0do8hcW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJHQu[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVAvPSCwTR?= NHLhdHE4PTN5M{Ox
human WiDr cells NYnvR5U3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV30dHZpUW6qaXLpeIlwdiCxZjDTRXAyOzBibXXkbYF1\WRiY3XscEBoem:5dHigbY4hcHWvYX6gW4lFeiClZXzsd{whUUN3ME2xNE46KG6P M365e|E4PjR|MUGy
human U251 cells MVvGeY5kfGmxbjDhd5NigQ>? MXrJcohq[mm2aX;uJI9nKFODUEGzNEBqdiCYRVfGMZN1cW23bHH0[YQhcHWvYX6gWVI2OSClZXzsd{BjgSCSTFHQJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9NVMvQCCwTR?= NGLMOJkyPzZ2M{GxNi=>

... Click to View More Cell Line Experimental Data

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
稳定性 powder
in solvent
别名 FR900506

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 (g) = 浓度 (mol/L) x 体积 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03194321 Recruiting End Stage Renal Disease Cedars-Sinai Medical Center|Astellas Pharma Inc May 9 2017 Phase 4
NCT02661035 Recruiting Acute Myelogenous Leukemia|Acute Lymphocytic Leukemia|Chronic Myelogenous Leukemia|Plasma Cell Leukemia|Myelodysplastic Syndromes|Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma|B-Cell Lymphoma|Follicular Lymphoma|Lymphoplasmacytic Lymphoma|Mantle-Cell Lymphoma|Prolymphocytic Leukemia|Lymphoblastic Lymphoma|Burkitt''s Lymphoma|Non-Hodgkin''s Lymphoma|Multiple Myeloma|Myeloproliferative Syndromes|Hematological Diseases Masonic Cancer Center University of Minnesota March 9 2017 Phase 2
NCT02723591 Recruiting Kidney Transplantation Astellas Pharma Global Development Inc.|Astellas Pharma Inc September 9 2016 Phase 4
NCT03277430 Recruiting Mayer Rokitansky Kuster Hauser Syndrome|Mullerian Aplasia|Uterus; Absence Congenital|Infertility Female|Uterus Absence Acquired|Absolute Uterine Factor Infertility Institute for Clinical and Experimental Medicine|University Hospital Motol|Sahlgrenska University Hospital Sweden October 9 2015 Phase 3
NCT01371331 Completed Kidney Transplantation|Heart Transplantation|Liver Transplantation Astellas Pharma Europe Ltd.|Astellas Pharma Inc June 9 2011 Phase 4
NCT03437577 Enrolling by invitation Kidney Transplant Failure and Rejection University of Minnesota - Clinical and Translational Science Institute May 8 2018 Phase 1|Phase 2

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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).

mTOR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID