Tacrolimus (FK506)
目录号：S5003 别名： FR900506
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。
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客户使用该产品的7个实验数据：
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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.
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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.
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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.
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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。 | ||||||||||||||||||||||||||||||||||||||||||||
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| 靶点 |
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| 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] |
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| Cell Data |
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| 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
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
*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
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 )
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。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
临床试验信息
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03603548 | Recruiting | Liver Transplant Rejection|Immunosuppression | Medical University of Warsaw | July 9 2018 | Not Applicable |
| NCT03194321 | Recruiting | End Stage Renal Disease | Cedars-Sinai Medical Center|Astellas Pharma Inc | May 9 2017 | Phase 4 |
| NCT02723591 | Recruiting | Kidney Transplantation | Astellas Pharma Global Development Inc.|Astellas Pharma Inc | September 9 2016 | Phase 4 |
| 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 |
| NCT03425071 | Recruiting | Kidney Transplantation|Rejection | University of Sao Paulo General Hospital|Maria da Luz Fernandes|Paschoalina Romano|Persio de Almeida Rezende Ebner|Nairo Massakazu Sumita|Veronica Porto Carreiro de Vasconcelos Coelho|Fabiana Agena|Elias David Neto|Nelson Zocoler Galante | March 8 2016 | -- |
技术支持
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如果有其他问题，请给我们留言。
常见问题及建议解决方法
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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?
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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).
