2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. nAChR 5-HT Receptor
  4. GTS-21 dihydrochloride

GTS-21 (dihydrochloride)  (Synonyms: DMXB-A; DMBX-anabaseine)

製品番号: HY-14564A 純度: 99.65%
COA 取扱説明書 Technical Support

GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti inflammatory and cognition enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist.

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CAS 番号 : 156223-05-1

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 66 在庫あり
Solution
10 mM * 1 mL in DMSO USD 66 在庫あり
Solid
5 mg $60 在庫あり
10 mg $96 在庫あり
50 mg $180 在庫あり
100 mg $280 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 14 publication(s) in Google Scholar

Other Forms of GTS-21 dihydrochloride:

GTS-21 (dihydrochloride) 関連抗体

Top Publications Citing Use of Products

    GTS-21 dihydrochloride purchased from MedChemExpress. Usage Cited in: Diabetologia. 2025 Dec 15.  [Abstract]

    HTR8/SVneo cells were treated with nicotine (NT), PNU or GTS-21 dihydrochloride (1 μM) at different concentrations (0, 0.1, 1, 10 μM) for 24 h under HG. Western blot images and quantification of p-p66Shc and p21 relative to GAPDH.

    GTS-21 dihydrochloride purchased from MedChemExpress. Usage Cited in: Diabetologia. 2025 Dec 15.  [Abstract]

    HTR8/SVneo cells or primary feeder cells were treated with normal glucose (NG), high glucose (HG), high glucose + PNU, or high glucose + GTS-21 dihydrochloride (1 μM), respectively. Mitochondrial membrane potential (MMP) was analyzed by flow cytometry using JC-1 staining.

    GTS-21 dihydrochloride purchased from MedChemExpress. Usage Cited in: Diabetologia. 2025 Dec 15.  [Abstract]

    HTR8/SVneo cells or primary trophoblast cells were treated with normal glucose (NG), high glucose (HG), high glucose + PNU, or high glucose + GTS-21 dihydrochloride (1 μM), respectively. Representative confocal microscopy images of mitochondrial permeability transition pore (mPTP) opening experiments quenched with calcein AM (green) and cobalt chloride (CoCl₂).

    GTS-21 dihydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2022 May:149:112733.

    GTS-21 dihydrochloride (10 μM). The relative expression levels of ZO-1, Occludin, and Claudin-1 in Caco2 cells were analyzed by Western blot.

    GTS-21 dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2022 Feb 8;8(1):54.  [Abstract]

    Intraperitoneal injection of GTS-21 (4 mg/kg) significantly downregulated the expression of NLRP3, ASC, Cl-Caspase-1 and GSDMD-N.

    5-HT Receptor アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

    • 生物活性

    • 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

    GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti inflammatory and cognition enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist[1][2].

    IC50 & Target[1][2]

    5-HT3A Receptor

     

    α7-nAChR

     

    human α4β2

    20 nM (Ki)

    5-HT3A Receptor

    3.1 μM (IC50)

    体外実験

    GTS-21 bound to human α4β2 nAChR (Ki=20 nM) 100-fold more potently than to humanα7-nAChR, and is 18- and 2-fold less potent than (-)-nicotine at human α4β2 and a7 nAChR, respectively[1].

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

    GTS-21 (dihydrochloride) 関連抗体
    体内実験

    GTS 21 (4 mg/kg; i.p.; 1, 3, 7, 14 and 21 days) reduces radiation induced histological signs of pulmonary injury[3].

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

    Animal Model: C57BL6 mice were irradiated with 12 Gy to induce a mouse model of Radiation induced lung injury (RILI)[3]
    Dosage: 4 mg/kg
    Administration: I.p.; 1, 3, 7, 14 and 21 days
    Result: Reduces lung inflammatory infiltrate and fibrosis in radiation treated mice.
    分子量

    381.30

    分子式

    C19H22Cl2N2O2
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    COC1=CC(OC)=CC=C1/C=C2CCCN=C\2C3=CC=CN=C3.Cl[H].Cl[H]
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    溶剤 & 溶解度
    体外: 

    H2O : 50 mg/mL (131.13 mM; Need ultrasonic)

    DMSO : 16.5 mg/mL (43.27 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6226 mL 13.1130 mL 26.2261 mL
    5 mM 0.5245 mL 2.6226 mL 5.2452 mL
    10 mM 0.2623 mL 1.3113 mL 2.6226 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    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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    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 (6.56 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 (6.56 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 75 mg/mL (196.70 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    純度とドキュメンテーション

    純度: 99.65%

    COA (255 KB) LCMS (118 KB)

    取扱説明書 (2659 KB)
    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 (sealed storage, away from moisture). 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
    DMSO / H2O 1 mM 2.6226 mL 13.1130 mL 26.2261 mL 65.5652 mL
    5 mM 0.5245 mL 2.6226 mL 5.2452 mL 13.1130 mL
    10 mM 0.2623 mL 1.3113 mL 2.6226 mL 6.5565 mL
    15 mM 0.1748 mL 0.8742 mL 1.7484 mL 4.3710 mL
    20 mM 0.1311 mL 0.6557 mL 1.3113 mL 3.2783 mL
    25 mM 0.1049 mL 0.5245 mL 1.0490 mL 2.6226 mL
    30 mM 0.0874 mL 0.4371 mL 0.8742 mL 2.1855 mL
    40 mM 0.0656 mL 0.3278 mL 0.6557 mL 1.6391 mL
    H2O 50 mM 0.0525 mL 0.2623 mL 0.5245 mL 1.3113 mL
    60 mM 0.0437 mL 0.2186 mL 0.4371 mL 1.0928 mL
    80 mM 0.0328 mL 0.1639 mL 0.3278 mL 0.8196 mL
    100 mM 0.0262 mL 0.1311 mL 0.2623 mL 0.6557 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    GTS-21 dihydrochloride Related Classifications

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    • 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）
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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.

    Keywords:

    GTS-21156223-05-1DMXB-A DMBX-anabaseineGTS21GTS 21nAChR5-HT ReceptorNicotinic acetylcholine receptorsSerotonin Receptor5-hydroxytryptamine Receptorpulmonaryinjuryfibrosislunganti inflammatorycognitionInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
    HY-14564A
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