Tacrolimus (FK506)

製品コード:S5003 別名:FR900506, Fujimycin, Prograf

For research use only.

Tacrolimus (FK506, FR900506, Fujimycin, Prograf) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.

Tacrolimus (FK506)化学構造

CAS No. 104987-11-3

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 25200
JPY 16900
JPY 73300
JPY 395400

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(73)

製品安全説明書

FKBP阻害剤の選択性比較

生物活性

製品説明 Tacrolimus (FK506, FR900506, Fujimycin, Prograf) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.
ターゲット
FKBP12 [1]
(T cells)
calcineurin [6]
体外試験

FK-506 and cyclosporin A block translocation of the cytoplasmic component without affecting synthesis of the nuclear subunit in T lymphocytes. [1] FK-506 prevents T-cell proliferation by inhibiting a Ca(2+)-dependent event required for induction of interleukin-2 transcription. [2] FK 506 binds to distinct families of intracellular proteins (immunophilins) termed cyclophilins and FK 506-binding proteins (FKBPs). FK-506 specifically inhibits cellular calcineurin at drug concentrations that inhibit interleukin 2 production in activated T cells. [3] FK-506 and CsA exert nearly identical biological effects in cells by inhibiting the same subset of early calcium-associated events involved in lymphokine expression, apoptosis, and degranulation. FK-506 binds to a family of intracellular receptors termed the FK-506 binding proteins (FKBPs). [4]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human U251 cells MVnGeY5kfGmxbjDhd5NigQ>? NWjFZ416UW6qaXLpeIlwdiCxZjDTRXAyOzBiaX6gWmVITi2|dHnteYxifGWmIHj1cYFvKFV{NUGgZ4VtdHNiYomgVGxCWCC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDJR|UxRTF|Lkigcm0> M3HkSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NkSzNVEzLz5zN{[0N|EyOjxxYU6=
human WiDr cells NWXVN|FmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVvJcohq[mm2aX;uJI9nKFODUEGzNEBu\WSrYYTl[EBk\WyuIHfyc5d1cCCrbjDoeY1idiCZaVTyJINmdGy|LDDJR|UxRTFyLkmgcm0> NXrk[nFqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe2OFMyOTJpPkG3OlQ{OTF{PD;hQi=>
human T-cell NV\oSGlkWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{fSU2lvKH[rdILvJIlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUMYNmdGxicILvcIln\XKjdHnvckwhUUN3ME2wMlUhdk1? M2ra[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493Nzd3M{ezN|EoRjd3M{ezN|E9N2F-
rat RBL2H3 cells NWCzd2xCTnWwY4Tpc44h[XO|YYm= Mon5NVUhdWmwcx?= NWjOd|BvSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiC{YYSgVmJNOkh|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTE6SLVLTRU1qdmS3Y3XkJHRPTi2jbIDoZUBxem:mdXP0bY9vKHC{ZXnuZ5Vj[XSnZDDmc5IhOTVibXnud{BxemmxcjDEUnAuSlODIHPoZYxt\W6pZTDt[YF{fXKnZDDh[pRmeiB|MDDtbY5{KGK7IFXMTXNCNCCLQ{WwQVAvOjVibl2= MmrWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2MUCwPFQoRjJ{NEGwNFg1RC:jPh?=
rat RBL2H3 cells NWLieolFTnWwY4Tpc44h[XO|YYm= NEfmNlAyPiCq NYfQWXZCUW6qaXLpeIlwdiCxZjDUUmYu[WyyaHGgdJJw\HWldHnvckBqdiC{YYSgVmJNOkh|IHPlcIx{KGGodHXyJFE3KGi{czDifUBGVEmVQTygTWM2OD1yLkK1JI5O NU\zcHIzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVExPzZpPkKzO|kyODd4PD;hQi=>
PBMCs NHLhTotHfW6ldHnvckBie3OjeR?= MWjJcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgTWZPNWejbX3hJJBzd2S3Y4Tpc44hMEGwdHmtR2Q{KG2xbn;jcI9v[WxiYX70bYJw\Hlic4TpcZVt[XSnZDDhcoQh[3WudIXy[YQhS0R2IIDvd4l1cX[nIHPlcIx{KHC3cnnmbYVlKG[{b32gbJVu[W5icHXybZBp\XKjbDDicI9w\CCvb37vcpVkdGWjcjDj[YxtMSxiSVO1NEA:KDBwMECwNFYh|ryPLh?= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTN4OUO5PUc,OTV|NkmzPVk9N2F-
PBMCs M{LabGZ2dmO2aX;uJIF{e2G7 NH;PXIVKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUUxvNTDwdo9lfWO2aX;uJEhCdnSrLVPEN{Bud26xY3zvcoFtKGGwdHnic4R6KHO2aX31cIF1\WRiYX7kJIN2dHS3cnXkJGNFPCCyb4PpeIl3\SClZXzsd{BxfXKrZnnl[EBnem:vIHj1cYFvKHCncnnwbIVz[WxiYnzvc4QhdW:wb371Z4xm[XJiY3XscEktKEmFNUCgQUAxNjByMEC2JO69VS5? MoDWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV|NkmzPVkoRjF3M{[5N|k6RC:jPh?=
T-cells M4TpfWZ2dmO2aX;uJIF{e2G7 M{S3Z3Rp\SClb33wc5Vv\CC5YYOgeIV{fGWmIH\vdkBqfHNiaX7obYJqfG:{eTDhZ5Rqfmm2eTDh[4FqdnO2IGStZ4VtdCCycn;sbYZmemG2aX;uJJV{cW6pIH31dolv\SC|cHzlcolkKFRvY3XscJMtKEmFNUCgQUAxNjByMEKg{txONg>? M1\6Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFyNEWwPVg4Lz5zMES1NFk5PzxxYU6=
RBL-2H3 MXTGeY5kfGmxbjDhd5NigQ>? MorBTY5pcWKrdHnvckBw\iCGTmC3MWJUSSCjboTp[4VvNWmwZIXj[YQhXE6IYXzwbIEhemWuZXHz[UBqdiC{YYSgVmJNNTKKMzDj[YxteyxiSVO1NEA:KDBwMECwNlUh|ryPLh?= NV70SpVPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[5NFE3QTZpPkG2PVAyPjl4PD;hQi=>
Jurkat T NXXIdFY3UW2vdX7vd5VxeHKnc4PpeoUh[XO|YYm= NXHib49qOTVidH:gN|AhdWmwcx?= M{\tcWludXWwb4P1dJBz\XO|aY\lJIFkfGm4aYT5JIlvKFCPQT;pc45wdXmlaX6gd5RqdXWuYYTl[EBpfW2jbjDKeZJs[XRiVDDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCLTEKgdJJw\HWldHnvckBxemW2cnXheIVlKG[xcjCxOUB1dyB|MDDtbY5{KG[xbHzve4VlKGK7IGDNRU9qd26xbYnjbY4h[WSmaYTpc44hdWWjc4Xy[YQh[W[2ZYKgNVghfG9iMkCgbJJ{KGK7IFXMTXNCNCCLQ{WwJF0hOC5|NjFOwG0v MnPEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2MUKyNFQoRjJ6NEGyNlA1RC:jPh?=
HEK293 M2\QRWZ2dmO2aX;uJIF{e2G7 Mkj4WHBgXFKDTmPQU3JVTVJ8IHnubIljcXSrb36gc4YhWGijbHzvbYRqdiC3cIThb4UhMFCqYXzsc4llcW58IEGgeW0qKGmwIF;BWHAuSy2neIDy[ZN{cW6pIFjFT|I6OyClZXzsd{whUUN3MDC9JFMvPyEQvF2u MofiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTR3M{C5NFcoRjF2NUOwPVA4RC:jPh?=
Jurkat T MoLHRY51cWmwZnzhcY1ifG:{eTDhd5NigQ>? MnvNNlAhdWmwcx?= NIHnclZCdnSrLXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCSTVGvbY9vd227Y3nuJJN1cW23bHH0[YQhcHWvYX6gTpVzc2G2IGSgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEmOLUKgd4VkemW2aX;uJJBz\WmwY4XiZZRm\CCob4KgNlAhdWmwczDmc4xtd3enZDDifUBRVUFxaX;uc416[2mwIIP0bY12dGG2aX;uJI1m[XO3cnXkJIFnfGW{IEGyJIhzeyCkeTDFUGlUSSxiSVO1NEA:KDVwODFOwG0v M2TOZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NUC5OVUzLz5{OEWwPVU2OjxxYU6=
アッセイ
Methods Test Index PMID
Western blot p-S6K(S371) / S6K / p-Erα(S167) / Erα ; p-JNK / JNK / p-ERK / ERK / Cytochrome c / cleaved caspase-3 ; GluA1 / pGluA1(S845) / GluA2 / GluA3 / Calcineurin 29344249 23470533 26455952
Immunofluorescence Tom20 / JC-1 / ROS / NF-κB ; FKBP51 ; FKBP52 / p23 / hsp90 30294901 20796173
Growth inhibition assay Cell viability 23470533
体内試験

FK-506 results in increase in the paw and tail withdrawal threshold as revealed by behavioral pain assessment in rats against hyperalgesic and allodynic stimuli. FK-506 also leads to a decrease in the serum nitrate and thiobarbituric acid reactive substance (TBARS) levels along with reduction in tissue myeloperoxidase (MPO) and total calcium levels, whereas, rise in tissue reduced glutathione levels in rats. FK-506 ameliorates the increase in the neuronal edema and axonal degeneration in rats with ischemia reperfusion (I/R). [5]

お薦めの試験操作(参考用のみ)

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+corn oil
混合させたのち直ちに使用することを推奨します。

15mg/mL

化学情報

分子量 804.02
化学式

C44H69NO12

CAS No. 104987-11-3
Storage 3年 -20°C
2年 -80°C in solvent
Smiles CC1CC(C2C(CC(C(O2)(C(=O)C(=O)N3CCCCC3C(=O)OC(C(C(CC(=O)C(C=C(C1)C)CC=C)O)C)C(=CC4CCC(C(C4)OC)O)C)O)C)OC)OC

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05432765 Not yet recruiting Other: Phenotypic Personalized Medicine Dosing Kidney Transplant Rejection University of Florida August 12 2022 Early Phase 1
NCT05005221 Recruiting Behavioral: Automated text messages Kidney Transplant University of Michigan July 11 2022 Not Applicable
NCT04505878 Recruiting Drug: Vitamin C Primary Graft Dysfunction|Lung Transplant; Complications University of Wisconsin Madison July 2022 Phase 2
NCT05316038 Not yet recruiting Diagnostic Test: Oral glucose tolerance test Kidney Transplant Infection|Cardiovascular Diseases|Immunosuppression|Kidney Transplant; Complications University Hospital Grenoble June 1 2022 --
NCT05260268 Not yet recruiting Behavioral: TEST Intervention Liver Transplant; Complications|Cirrhosis|End Stage Liver DIsease|Medication Adherence University of Pennsylvania|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) June 1 2022 Not Applicable
NCT05439941 Enrolling by invitation Drug: EDP1815 Atopic Dermatitis Evelo Biosciences Inc. June 6 2022 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

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よくある質問(FAQ)

質問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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