2. Immunology/Inflammation
  3. Aryl Hydrocarbon Receptor
  4. Tapinarof

タピナロフ  (Synonyms: Tapinarof; WBI-1001; Benvitimod; GSK2894512)

製品番号: HY-109044 純度: 99.95%
COA 取扱説明書 Technical Support

Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice.

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CAS 番号 : 79338-84-4

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 在庫あり
Solution
10 mM * 1 mL in DMSO USD 55 在庫あり
Solid
5 mg $50 在庫あり
10 mg $80 在庫あり
25 mg $155 在庫あり
50 mg $250 在庫あり
100 mg $400 在庫あり
250 mg $800 在庫あり
500 mg   お問い合わせ  
1 g   お問い合わせ  

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カスタマーレビュー

Based on 15 publication(s) in Google Scholar

Other Forms of Tapinarof:

タピナロフ 関連抗体

Top Publications Citing Use of Products

    Tapinarof purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2025 Jun 17;122(24):e2424985122.  [Abstract]

    Quantitative proteomics (TMT 18-plex) volcano plots showing significantly upregulated (red) and downregulated (blue) proteins in HCC44 cells treated with 1 μM Tapinarof (24 h).

    Tapinarof purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2025 Jun 17;122(24):e2424985122.  [Abstract]

    Western blotting analysis of AHR and SOCS3 levels in HCC44 cells treated with 1 µM RBN2397 with or without 1 µM CH223191 and 1 µM Tapinarof (24 h).

    Tapinarof purchased from MedChemExpress. Usage Cited in: EMBO J. 2026 Jan;45(1):261-277.  [Abstract]

    HCC44 cells were pre-treated with DMSO, 1 µM Tapinarof and PARP inhibitors (PARP1/2 (1 µM Olaparib), PARP7 (100 nM RBN2397), PARP14 (200 nM RBN012759), TNKS (1 µM AZ6102)) for 20 h followed by an additional 4 h of 1 µM TAK243 or 10 µM MG132 treatment.

    Tapinarof purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Oct:46:102110.

    CYP1A1 enzyme activity measurement in HaCaT cells and NHEKs treated for 24 h with 100 nM Tapinarof (n = 3).

    Tapinarof purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Oct:46:102110.

    CYP1A1 enzyme activity measurement in HaCaT cells and NHEKs treated for 24 h with 100 nM Tapinarof (n = 3).

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    製品説明

    Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice[1].

    IC50 & Target

    EC50: 13 nM (AhR)[1]
    Cellular Effect
    Cell Line Type Value Description References
    CD4+ve Th IC50
    5.2 3
    Compound: Tapi
    Induction of apoptosis in human CD4+ve Th cells
    Induction of apoptosis in human CD4+ve Th cells
    		[PMID: 35123295]
    CD4+ve Th IC50
    5.2 3
    Compound: Tapi
    Induction of apoptosis in human CD4+ve Th cells
    Induction of apoptosis in human CD4+ve Th cells
    		[PMID: 35123295]
    体外実験

    Tapinarof activates the AhR pathway through direct binding. Tapinarof dose-dependently induces nuclear translocation of AhR in immortalized keratinocytes (HaCaT) (EC50=0.16 nM)[1].

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

    タピナロフ 関連抗体
    体内実験

    Tapinarof acts through AhR to reduce inflammation in IMQ-treated mice. AhR-sufficient mice on a C57Bl/6 background exhibit a reduced clinical score after treatment with Tapinarof or 6-formylindolo(3,2-b)carbazole (FICZ). In contrast, AhR KO mice do not respond to the anti-inflammatory effects of Tapinarof. FICZ is used as a comparator in these studies and yields similar results, with dramatically reduced inflammatory responses in wild-type, but not AhR KO mice[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    254.32

    分子式

    C17H18O2
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    OC1=C(C(C)C)C(O)=CC(/C=C/C2=CC=CC=C2)=C1
    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: 

    Ethanol : ≥ 100 mg/mL (393.21 mM)

    DMSO : 100 mg/mL (393.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.9321 mL 19.6603 mL 39.3205 mL
    5 mM 0.7864 mL 3.9321 mL 7.8641 mL
    10 mM 0.3932 mL 1.9660 mL 3.9321 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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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

    濃度 （開始）

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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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (9.83 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (9.83 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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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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    +
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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, 1 year; -20°C, 6 months (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: 99.95%

    COA (247 KB) HNMR (243 KB) RP-HPLC (255 KB) MS (238 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [1]

    HaCaT cells (10,000 cells/well) are cultured in 96-well Greiner μCLEAR plates in 100 μL DMEM with HEPES, Glutamax and 10% fetal bovine serum to confluence. Media is replaced with 100 μL media containing 0.2% heat-inactivated, charcoal-stripped fetal bovine serum and incubated overnight. Titrating concentrations of Tapinarof (10-8 μM ,10-6 μM, 10-4 μM, 0.01 μM, and 1 μM) are added for 30 minutes followed by washing and fixing in ice-cold methanol:acetone (50:50). Samples are blocked with 3% BSA for 1 hour, and then washed again in phosphate buffered saline with 0.1% Tween-20. Next, cells are stained with 50 μL of 1:50 dilution anti-AhR antibody in 3% BSA, followed by 50 μL secondary antibody (1:500 dilution chicken anti-rabbit AlexaFluor488 and 1:2,000 dilution Hoechst 33342) in 3% BSA/phosphate buffered saline. Images are acquired on InCell 2000 and/or Opera. Image analysis is performed using InCell Analyzer Workstation and/or Columbus[1].

    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
    [1]

    Mice[1]
    Female BALB/c mice (BALB/cByJRj) are used. Studies are performed using 100 µL of Tapinarof (1%) or FICZ (0.01%, at the limit of solubility) in 60% ethanol: 40% water[1].

    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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 3.9321 mL 19.6603 mL 39.3205 mL 98.3013 mL
    5 mM 0.7864 mL 3.9321 mL 7.8641 mL 19.6603 mL
    10 mM 0.3932 mL 1.9660 mL 3.9321 mL 9.8301 mL
    15 mM 0.2621 mL 1.3107 mL 2.6214 mL 6.5534 mL
    20 mM 0.1966 mL 0.9830 mL 1.9660 mL 4.9151 mL
    25 mM 0.1573 mL 0.7864 mL 1.5728 mL 3.9321 mL
    30 mM 0.1311 mL 0.6553 mL 1.3107 mL 3.2767 mL
    40 mM 0.0983 mL 0.4915 mL 0.9830 mL 2.4575 mL
    50 mM 0.0786 mL 0.3932 mL 0.7864 mL 1.9660 mL
    60 mM 0.0655 mL 0.3277 mL 0.6553 mL 1.6384 mL
    80 mM 0.0492 mL 0.2458 mL 0.4915 mL 1.2288 mL
    100 mM 0.0393 mL 0.1966 mL 0.3932 mL 0.9830 mL
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    Tapinarof Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      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.

    Keywords:

    Tapinarof79338-84-4WBI-1001 Benvitimod GSK2894512WBI1001WBI 1001GSK2894512GSK 2894512GSK-2894512Aryl Hydrocarbon ReceptorAhRInhibitorinhibitorinhibit

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    製品名:
    Tapinarof
    製品番号:
    HY-109044
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