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  4. Tacrolimus

タクロリムス  (Synonyms: FK506; Tacrolimus; Fujimycin)

製品番号: HY-13756 純度: 99.93%
COA 取扱説明書 Technical Support

Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 104987-11-3

容量 価格(税別) 在庫状況 数量
5 mg $32 在庫あり
10 mg $50 在庫あり
50 mg $84 在庫あり
100 mg $126 在庫あり
200 mg $180 在庫あり
500 mg $312 在庫あり
1 g $450 在庫あり
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カスタマーレビュー

Based on 101 publication(s) in Google Scholar

Other Forms of Tacrolimus:

Top Publications Citing Use of Products

顧客検証

IF
ELISA
Flow Cytometry
WB

    Tacrolimus purchased from MedChemExpress. Usage Cited in: Toxics. 2024 Aug 19;12(8):607.  [Abstract]

    Tacrolimus monohydrate (100 nM-10 µM) decreased IL-2 secretion from Jurkat cells and coculture with THP-1 cells.

    Tacrolimus purchased from MedChemExpress. Usage Cited in: Toxics. 2024 Aug 19;12(8):607.  [Abstract]

    Tacrolimus monohydrate (100 nM-10 µM) caused significant TNFα inhibition in Jurkat cells and coculture with THP-1 cells.

    Tacrolimus purchased from MedChemExpress. Usage Cited in: Toxics. 2024 Aug 19;12(8):607.  [Abstract]

    Tacrolimus monohydrate (100 nM-10 µM) significantly inhibited IL-8 secretion from THP-1, Jurkat cells and their coculture.

    Tacrolimus purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2023 Oct;56(10):e13460.  [Abstract]

    FK506 (5 μM; 14 days) significantly inhibits the protein expression of both calcineurin A and NFATC2 in hLESCs.

    Tacrolimus purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2023 Oct;56(10):e13460.  [Abstract]

    FK506 (5 μM; 14 days) inhibits WNT16b on hLESC cell proliferation.

    Tacrolimus purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2023 Oct;56(10):e13460.  [Abstract]

    FK506 (5 μM; 14 days) significantly inhibits the expression of WNT16b-promoting cell proliferation marker Ki67 and the putative hLESC marker ΔNp63α in hLESCs.

    Tacrolimus purchased from MedChemExpress. Usage Cited in: SSRN. 2023 Oct 31.

    Tacrolimus monohydrate (FK506) (100 ng/mL) significantly increased the expressions of protein K14, CDH1 in kCSTA cells in an inflammatory environment.

    Tacrolimus purchased from MedChemExpress. Usage Cited in: SSRN. 2023 Oct 31.

    Tacrolimus monohydrate (FK506) (100 ng/mL) increased CSTA proteins in kCSTA cells.

    Tacrolimus purchased from MedChemExpress. Usage Cited in: Cell Biol Toxicol. 2022 Jun;38(3):487-504.  [Abstract]

    FK506 inhibits dephosphorylation of Drp-1 at Ser637 site induced by CVB3 infection. CVB3 infection-induced decrease in Bcl-2 expression and enhanced levels of Bax and Caspase-3 cleavage are reversed by FK506.

    Tacrolimus purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2019 Dec 27;9(1):1709262.  [Abstract]

    Exosomal PD-L1 suppressed T cell activation and promoted skin cell migration in vitro (a). Representative confocal image show the appearance of exosomes as small-red dots. (b-c). Representative confocal images of pre-stained exosomes (red) colocalized with cell membrane (green) of HEK 293T (b) and Jurkat T cells (c).

    Tacrolimus purchased from MedChemExpress. Usage Cited in: Brain Res. 2019 May 15:1711:68-76.  [Abstract]

    Levels of CytC in cytosol (Cyto-CytC), CytC in mitochondria (Mito- CytC) and cleaved caspase-3 in hippocampus are determined by western blot with the treatment of sham, HIR, MDV or FK506.

    Tacrolimus purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jan 1;8(4):878-893.  [Abstract]

    Accumulation of immune cells in host mice. Immunofluorescent images of CD4+ cells (green) in transplanted site in the normal, E+R, E+R+T, and E+R+T-RNPs groups at day 7 and day 21.
    • 生物活性

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    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties[1].

    IC50 & Target

    Macrolide

     

    Cellular Effect
    Cell Line Type Value Description References
    B-cell IC50
    1.6 x 10-3 μg/mL
    Compound: FK-506
    Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
    Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
    [PMID: 14738397]
    CD4+ve Th IC50
    0.034 nM
    Compound: 1; FK506
    Immunosuppressive activity in C57BL/6J mouse CD4+ve T cells assessed as inhibition of CD3/CD28-stimulated CD4+ve T cell proliferation incubated for 72 hrs by CellTrace-violet staining based flow cytometry analysis
    Immunosuppressive activity in C57BL/6J mouse CD4+ve T cells assessed as inhibition of CD3/CD28-stimulated CD4+ve T cell proliferation incubated for 72 hrs by CellTrace-violet staining based flow cytometry analysis
    [PMID: 33534559]
    HEK293 IC50
    3.7 μM
    Compound: FK506
    TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells
    TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells
    [PMID: 14530907]
    HepG2 IC50
    > 100 μM
    Compound: 1; FK-506
    Cytotoxicity against human HepG2 cells
    Cytotoxicity against human HepG2 cells
    [PMID: 28412204]
    Jurkat IC50
    0.056 nM
    Compound: 1, FK506
    Inhibition of calcineurin in human Jurkat cells assessed as inhibition of NFAT-mediated IL-2 production after 8 hrs by beta-lactamase reporter gene assay
    Inhibition of calcineurin in human Jurkat cells assessed as inhibition of NFAT-mediated IL-2 production after 8 hrs by beta-lactamase reporter gene assay
    10.1039/C2MD20266B
    Jurkat IC50
    0.19 nM
    Compound: FK-506
    Inhibitory activity against IL-2 receptor in human T-cell jurkat cell line stimulated by phytohemagglutininin and phorbol myristate acetate
    Inhibitory activity against IL-2 receptor in human T-cell jurkat cell line stimulated by phytohemagglutininin and phorbol myristate acetate
    [PMID: 15369399]
    Jurkat IC50
    0.36 μM
    Compound: 1; FK-506
    Immunosuppressive activity in PMA/ionomycin stimulated human Jurkat T cells assessed as suppression of IL2 production pretreated for 15 to 30 mins followed by PMA/ionomycin addition measured after 18 to 20 hrs by ELISA
    Immunosuppressive activity in PMA/ionomycin stimulated human Jurkat T cells assessed as suppression of IL2 production pretreated for 15 to 30 mins followed by PMA/ionomycin addition measured after 18 to 20 hrs by ELISA
    [PMID: 28412204]
    Jurkat IC50
    5.8 μM
    Compound: FK506
    Anti-inflammatory activity in PMA/ionomycin stimulated human Jurkat T cells assessed as reduction in IL-2 secretion preincubated for 20 mins followed by PMA/ionomycin stimulation measured after 12 hrs by ELISA
    Anti-inflammatory activity in PMA/ionomycin stimulated human Jurkat T cells assessed as reduction in IL-2 secretion preincubated for 20 mins followed by PMA/ionomycin stimulation measured after 12 hrs by ELISA
    [PMID: 28509552]
    PBMC IC50
    0.29 nM
    Compound: FK-506
    Inhibitory activity against murine mixed lymphocyte reaction
    Inhibitory activity against murine mixed lymphocyte reaction
    [PMID: 15369399]
    RBL-2H3 IC50
    0.25 nM
    Compound: FK-506
    Inhibition of DNP7-BSA antigen-induced TNFalpha release in rat RBL-2H3 cells
    Inhibition of DNP7-BSA antigen-induced TNFalpha release in rat RBL-2H3 cells
    [PMID: 16901696]
    RBL-2H3 IC50
    0.25 nM
    Compound: FK-506
    Antiinflammatory activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced TNF-alpha production preincubated for 15 mins prior DNP-BSA challenge measured after 30 mins by ELISA
    Antiinflammatory activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced TNF-alpha production preincubated for 15 mins prior DNP-BSA challenge measured after 30 mins by ELISA
    [PMID: 22410084]
    RBL-2H3 IC50
    0.25 nM
    Compound: FK506
    Inhibition of TNF-alpha production in rat RBL2H3 cells after 16 hrs by ELISA
    Inhibition of TNF-alpha production in rat RBL2H3 cells after 16 hrs by ELISA
    [PMID: 23791076]
    T-cell IC50
    0.18 nM
    Compound: 1 (FK-506)
    Agonistic activity in a murine splenic T-cell proliferation assay was calculated by measurement of [3H]thymidine uptake relative to control
    Agonistic activity in a murine splenic T-cell proliferation assay was calculated by measurement of [3H]thymidine uptake relative to control
    10.1016/S0960-894X(01)81248-8
    T-cell IC50
    0.29 nM
    Compound: 1 (FK-506)
    In vitro evaluation for immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells
    In vitro evaluation for immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells
    10.1016/S0960-894X(01)80264-X
    T-cell IC50
    0.29 nM
    Compound: 1 (FK-506)
    In vitro immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells
    In vitro immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells
    10.1016/S0960-894X(01)80265-1
    T-cell IC50
    0.5 nM
    Compound: FK-506
    In vitro inhibitory activity against human T-cell proliferation.
    In vitro inhibitory activity against human T-cell proliferation.
    [PMID: 7537331]
    T-cell IC50
    0.9 nM
    Compound: FK-506
    In vitro inhibitory activity against human T-cell production of lymphokine IL-2
    In vitro inhibitory activity against human T-cell production of lymphokine IL-2
    [PMID: 7537331]
    T-cell IC50
    1.5 x 10-5 μg/mL
    Compound: FK-506
    Immunosuppressant activity in mouse T cells assessed as inhibition of concanavalin A-induced cell proliferation
    Immunosuppressant activity in mouse T cells assessed as inhibition of concanavalin A-induced cell proliferation
    [PMID: 11575965]
    T-cell IC50
    1.5 x 10-5 μg/mL
    Compound: FK-506
    Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
    Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
    [PMID: 14738397]
    U-251 IC50
    13.8 nM
    Compound: 1
    Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay
    Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay
    [PMID: 17643112]
    Vero 76 IC50
    > 100 μM
    Compound: 1; FK-506
    Cytotoxicity against African green monkey Vero 76 cells
    Cytotoxicity against African green monkey Vero 76 cells
    [PMID: 28412204]
    WiDr IC50
    10.9 nM
    Compound: 1
    Inhibition of SAP130 mediated cell growth in human WiDr cells
    Inhibition of SAP130 mediated cell growth in human WiDr cells
    [PMID: 17643112]
    体外実験

    Tacrolimus (FK506) inhibits calcium-dependent events, such as IL-2 gene transcription, NO synthase activation, cell degranulation, and apoptosis. Tacrolimus also potentiates the actions of glucocorticoids and progesterone by binding to FKBPs contained within the hormone receptor complex, preventing degradation. The agent may enhance expression of the TGFβ-1 gene in a fashion analogous to that demonstrated for CsA. T cell proliferation in response to ligation of the T cell receptor is inhibited by Tacrolimus[1]. Treatment with a low concentration of Tacrolimus (FK506,10 μg/L) does not significantly affect the proliferation of MH3924A cells (P=0.135). Upon treatment with higher concentrations of Tacrolimus (100-1,000 μg/L), the proliferation of MH3924A cells is significantly enhanced (P<0.01). Treatment with AMD3100 at any concentration (10, 50 or 100 μg/L), has no obvious effect on MH3924A cell proliferation (P>0.05). However, when different concentrations of AMD3100 are combined with 100 μg/L Tacrolimus, the in vitro proliferation of MH3924A cells is increased (P<0.01)[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    体内実験

    The therapeutic effect of Tacrolimus is investigated on progression and perpetuation of colitis by administering Tacrolimus to Dextran sulfate sodium (DSS)-treated mice from Days 10 to 16 or to 23. At Days 17 and 24, colon length is significantly shortened, and colon weight is significantly higher in DSS-treated control animals than in normal animals. In addition, colon weight per unit length in the control group is more than twice that in the normal group. While both 7 and 14 d treatment with Tacrolimus significantly suppresses increases in colon weight per unit length in DSS-treated animals compared with the control group, this treatment does not actually restore the colon shortening. In addition, this inhibitory effect of Tacrolimus on increases in colon weight per unit length is more pronounced with 14-d than 7-d treatment, as shown by the inhibitory percentages (59% vs. 28%)[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    臨床実験
    分子量

    804.02

    分子式

    C44H69NO12

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@@](CCCC1)([H])N1C(C([C@@]2(O)[C@H](C)C[C@H](OC)[C@@](O2)([H])[C@@H](OC)C[C@@H](C)C/C(C)=C/[C@H]3CC=C)=O)=O)O[C@H](/C(C)=C/[C@H]4C[C@@H](OC)[C@H](O)CC4)[C@H](C)[C@@H](O)CC3=O

    Structure Classification
    Initial Source

    fungus Streptomyces tsukubaensis.

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶剤 & 溶解度
    体外: 

    DMSO : 125 mg/mL (155.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 12.5 mg/mL (15.55 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.2438 mL 6.2188 mL 12.4375 mL
    5 mM 0.2488 mL 1.2438 mL 2.4875 mL
    10 mM 0.1244 mL 0.6219 mL 1.2438 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    一般には略語で表示されます:C1V1 = C2V2

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.75 mg/mL (3.42 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.93%

    参考文献
    細胞実験
    [3]

    Tumor cell proliferation is determined by the MTT assay. Briefly, after MH3924A cells have reached the logarithmic growth phase, a 0.2-mL cell suspension at 1×104 cells/mL is added into each well of a 96-well plate and cultured in DMEM for 24 h. When adherent growth is established, different concentrations of Tacrolimus (10, 100 and 1,000 μg/L) , AMD3100 (10, 50 and 100 μg/L) and Tacrolimus (0 and 100 μg/L)+AMD3100 (0, 10, 50 and 100 μg/L) are added into the plates. Untreated cells cultured in medium alone are used as controls. After culturing for 48 h, 10 μL MTT (5 g/L) are added, and each well is incubated for 6 h; next, 150 μL/well DMSO are added, followed by measurements of the absorbance at 570 mm on a spectrophotometer reader. Each well is measured three times, and each sample is assayed in triplicate[3].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [4]

    Mice[4]
    Six-week-old male C57BL/6J mice are maintained in a temperature- and humidity-controlled room with a 12-h light-dark cycle. For the multiple dosing study, colitic mice (n=10) are orally administered Tacrolimus at 30 mg/kg for 7 d (Days 10 to 16) or 14 d (Days 10 to 23). Control (n=10) and normal groups (n=5) are administered placebo using the same regimen. Tacrolimus or placebo is administered at 10 mL/kg. Mice are euthanized by CO2 inhalation on the day following the final dosing. For the single dosing study, colitic mice are orally administered Tacrolimus at 30 mg/kg or placebo (n=8) once on Day 7, 10, 17, or 24. Normal mice (n=4) are administered placebo using the same regimen. Mice are euthanized by CO2 inhalation eight hours after dosing[4].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 1.2438 mL 6.2188 mL 12.4375 mL 31.0938 mL
    5 mM 0.2488 mL 1.2438 mL 2.4875 mL 6.2188 mL
    10 mM 0.1244 mL 0.6219 mL 1.2438 mL 3.1094 mL
    15 mM 0.0829 mL 0.4146 mL 0.8292 mL 2.0729 mL
    DMSO 20 mM 0.0622 mL 0.3109 mL 0.6219 mL 1.5547 mL
    25 mM 0.0498 mL 0.2488 mL 0.4975 mL 1.2438 mL
    30 mM 0.0415 mL 0.2073 mL 0.4146 mL 1.0365 mL
    40 mM 0.0311 mL 0.1555 mL 0.3109 mL 0.7773 mL
    50 mM 0.0249 mL 0.1244 mL 0.2488 mL 0.6219 mL
    60 mM 0.0207 mL 0.1036 mL 0.2073 mL 0.5182 mL
    80 mM 0.0155 mL 0.0777 mL 0.1555 mL 0.3887 mL
    100 mM 0.0124 mL 0.0622 mL 0.1244 mL 0.3109 mL
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます:C1V1 = C2V2

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    × = ×
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    製品名:
    Tacrolimus
    製品番号:
    HY-13756
    数量:
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