2. Anti-infection Cell Cycle/DNA Damage
  3. Antibiotic Bacterial Topoisomerase
  4. Gepotidacin

Gepotidacin  (Synonyms: GSK2140944)

製品番号: HY-16742 純度: 99.92%
COA 取扱説明書 Technical Support

Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.

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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 : 1075236-89-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 462 在庫あり
Solution
10 mM * 1 mL in DMSO USD 462 在庫あり
Solid
1 mg $132 在庫あり
5 mg $420 在庫あり
10 mg $720 在庫あり
25 mg $1460 在庫あり
50 mg $2340 在庫あり
100 mg $3360 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

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 12 publication(s) in Google Scholar

Other Forms of Gepotidacin:

Gepotidacin 関連抗体

Top Publications Citing Use of Products

    Gepotidacin purchased from MedChemExpress. Usage Cited in: Antimicrob Agents Chemother. 2026 Apr;70(4):e0170625.

    In vitro induction of Gepotidacin (18-24 h) resistance in N. gonorrhoeae ST8123 occurred. MZX-24-16 (ST8123 isolate with GyrA S91F/D95A and ParC E91G) was used.

    Gepotidacin purchased from MedChemExpress. Usage Cited in: ACS Infect Dis. 2026 Jan 9;12(1):363-375.  [Abstract]

    Gepotidacin induced primarily single-stranded DNA breaks mediated by B. anthracis gyrase.

    Gepotidacin purchased from MedChemExpress. Usage Cited in: Antibiotics (Basel). 2022 Feb 1;11(2):192.

    MIC (mg/L) distribution of N = 100 Stenotrophomonas maltophilia strains for Gepotidacin as found in broth microdilution after EUCAST.

    Gepotidacin purchased from MedChemExpress. Usage Cited in: Microbiol Spectr. 2022 Dec 21;10(6):e0205622.  [Abstract]

    Time-kill kinetics of the novel bacterial topoisomerase inhibitor (NBTI) compound Gepotidacin and comparator agents for S. aureus were assessed.Untreated time (T) of 0 h, 1.67 × 106 CFU/mL; untreated T of 24 h, 3.66 × 109 CFU/mL.

    Gepotidacin purchased from MedChemExpress. Usage Cited in: Cell Chem Biol. 2019 Sep 19;26(9):1274-1282.e4.  [Abstract]

    Cross-Resistance of EN-7R Strains with Other Gyrase Inhibitors
    No observed cross-resistance between EN-7 and other gyrase-targeting antibiotics, ciprofloxacin and novobiocin; however, there is some cross-resistance to the NBTI Gepotidacin.

    Antibiotic 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
    Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

    Topoisomerase 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
    Topoisomerase Topo I Topo II DNA gyrase

    • 生物活性

    • プロトコル

    • 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

    Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.

    Cellular Effect
    Cell Line Type Value Description References
    HepG2 IC50
    >128 6
    Compound: GEP
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability for 24 hrs by Celltiter-Glo assay
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability for 24 hrs by Celltiter-Glo assay
    		[PMID: 35231579]
    HepG2 IC50
    > 128 6
    Compound: GEP
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability for 24 hrs by Celltiter-Glo assay
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability for 24 hrs by Celltiter-Glo assay
    		[PMID: 35231579]
    HepG2 IC50
    > 128 6
    Compound: GEP
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability for 24 hrs by Celltiter-Glo assay
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability for 24 hrs by Celltiter-Glo assay
    		[PMID: 35231579]
    体外実験

    Gepotidacin is a novel, first-in-class, triazaacenaphthylene antibacterial that inhibits bacterial DNA gyrase and topoisomerase IV via a unique mechanism and has demonstrated in vitro activity against gram-negative and gram-positive bacterias , including drug-resistant strains, and also targets pathogens associated with other conventional and biothreat infections. The MIC50 and MIC90 for gepotidacin against the 25 N. gonorrhoeae isolates tested are 0.12 and 0.25 μg/mL, respectively[1]. The gepotidacin MIC90s are as follows (in μg/mL): Streptococcus pyogenes, 0.25; Escherichia coli, 2; Moraxella catarrhalis, ≤0.06; Streptococcus pneumoniae, 0.25; Haemophilus influenzae, 1; Clostridium perfringens, 0.5; and Shigella spp., 1[2]. Gepotidacin hasin vitroactivity against causative pathogens of acute bacterial skin and skin structure infections (ABSSSIs)[3].

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

    Gepotidacin 関連抗体
    体内実験

    GSK2140944 MICs are 0.125 to 0.5 mg/L against the six MRSA isolates. ELF penetration ratios range from 1.1 to 1.4. Observed maximal decreases are 1.1 to 3.1 log10 CFU in neutropenic mice. The mean fAUC/MIC ratios required for stasis and 1-log-unit decreases are 59.3 ± 34.6 and 148.4 ± 83.3, respectively.

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

    448.52

    分子式

    C24H28N6O3
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(C=NC(C=C1)=C23)N3[C@H](CN4CCC(NCC5=CC(CCCO6)=C6C=N5)CC4)CN2C1=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 7.14 mg/mL (15.92 mM; Need ultrasonic; 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 2.2296 mL 11.1478 mL 22.2956 mL
    5 mM 0.4459 mL 2.2296 mL 4.4591 mL
    10 mM 0.2230 mL 1.1148 mL 2.2296 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    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）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    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: ≥ 0.71 mg/mL (1.58 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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: ≥ 0.71 mg/mL (1.58 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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:

    Dosage

    mg/kg

    Animal weight
    (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.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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).
    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: 99.92%

    COA (253 KB) HNMR (492 KB) RP-HPLC (254 KB) LCMS (97 KB)

    取扱説明書 (2659 KB)
    参考文献
    動物実験
    [4]

    Mice: For neutropenic pharmacokinetic studies, at 3 h postinoculation (0 h), groups of 48 infected mice are administered GSK2140944 s.c. in single doses of 6.25, 50, or 200 mg/kg. Blood samples are collected from groups of six mice at 5 min and 0.25, 0.5, 1, 1.5, 2, 3, and 4 h postdose for 6.25- or 50-mg/kg doses and 5 min and 0.25, 0.5, 1, 1.5, 2, 4, and 6 h postdose for the 200-mg/kg dose via cardiac puncture[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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2296 mL 11.1478 mL 22.2956 mL 55.7389 mL
    5 mM 0.4459 mL 2.2296 mL 4.4591 mL 11.1478 mL
    10 mM 0.2230 mL 1.1148 mL 2.2296 mL 5.5739 mL
    15 mM 0.1486 mL 0.7432 mL 1.4864 mL 3.7159 mL
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    Gepotidacin Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    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:

    Gepotidacin1075236-89-3GSK2140944GSK 2140944GSK-2140944AntibioticBacterialTopoisomeraseInhibitorinhibitorinhibit

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    製品名:
    Gepotidacin
    製品番号:
    HY-16742
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