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

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

For research use only. We do not sell to patients.

CAS No. : 1075236-89-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Gepotidacin:

Gepotidacin Related Antibodies

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.

    View All Antibiotic Isoform Specific Products:

    View All Isoforms
    Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

    View All Topoisomerase Isoform Specific Products:

    View All Isoforms
    Topoisomerase Topo I Topo II DNA gyrase

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    Cellular Effect
    Cell Line Type Value Description References
    HepG2 IC50
    > 128 μg/mL
    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]
    In Vitro

    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 Related Antibodies
    In Vivo

    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.
    Clinical Trial
    Molecular Weight

    448.52

    Formula

    C24H28N6O3
    CAS No.
    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    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
    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
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.
    Purity & Documentation

    Purity: 99.92%

    SDS (393 KB)

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

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [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].

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

    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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Gepotidacin Related Classifications

    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

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Gepotidacin
    Cat. No.:
    HY-16742
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB) Italian - IT (393 KB) Korean - KR (393 KB) Portuguese - PT (393 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.