Art. -Nr.: HY-16742

Gepotidacin

Name: Gepotidacin
Brand: MedChemExpress
SKU: HY-16742
Price: 55.00 USD
Availability: InStock
Rating: 5 (12 reviews)

(Synonyms: GSK2140944)

12 Cited Publications

Kundenbewertung

Based on 12 publication(s) in Google Scholar

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

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.92%
CAS. Nr.: 1075236-89-3
Formel: C₂₄H₂₈N₆O₃
Molecular Weight:448.52

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Gepotidacin Chemical Structure

CAS. Nr.: 1075236-89-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Alle Antibiotic Isoform-spezifische Produkte anzeigen :

Alle Topoisomerase Isoform-spezifische Produkte anzeigen :

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. .

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1075236-89-3
Appearance Solid
Molecular Weight 448.52
Formel C₂₄H₂₈N₆O₃
Color White to yellow
SMILES

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

GSK2140944
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

All Gel ElectrophoresisMicrobiological Assay

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Journal Impact Factor

Nat Microbiol

Characterization of antibiotic resistomes by reprogrammed bacteriophage-enabled functional metagenomics in clinical strains. [Abstract]

2023 Mar;8(3):410-423. PMID: 36759752
Cell Chem Biol

Discovery of a Novel DNA Gyrase-Targeting Antibiotic through the Chemical Perturbation of Streptomyces venezuelae Sporulation. [Abstract]

2019 Sep 19;26(9):1274-1282.e4. PMID: 31279606

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

Cross-Resistance of EN-7^R 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.
PLoS Biol

Rational design of balanced dual-targeting antibiotics with limited resistance. [Abstract]

2020 Oct 5;18(10):e3000819. PMID: 33017402
Antibiotics (Basel)

Antibacterial Activity of the Novel Drug Gepotidacin against Stenotrophomonas maltophilia-An In Vitro and In Vivo Study. [Abstract]

2022 Feb 1;11(2):192. PMID: 35203795

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

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

Activities of the Novel Bacterial Topoisomerase Inhibitor OSUAB-0284 against the Biothreat Pathogen Bacillus anthracis and Its Type II Topoisomerases. [Abstract]

2026 Jan 9;12(1):363-375. PMID: 41430688

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.
ACS Infect Dis

Role of DNA Double-Strand Break Formation in Gyrase Inhibitor-Mediated Killing of Nonreplicating Persistent Mycobacterium tuberculosis in Caseum. [Abstract]

2024 Oct 11;10(10):3631-3639. PMID: 39315541
Antimicrob Agents Chemother

Stepwise evolution and clonal enrichment of gepotidacin resistance in Neisseria gonorrhoeae. [Abstract]

2026 Apr;70(4):e0170625. PMID: 41810969

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

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.
Antimicrob Agents Chemother

Multidrug tolerance conferred by loss-of-function mutations in anti-sigma factor RshA of Mycobacterium abscessus. [Abstract]

2024 Dec 5;68(12):e0105124. PMID: 39470195
Microbiol Spectr

Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors Exhibit Bactericidal Activity against Planktonic and Biofilm Staphylococcus aureus In Vitro. [Abstract]

2022 Dec 21;10(6):e0205622. PMID: 36250857

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.
Vet Microbiol

Antibacterial activity of novel bacterial topoisomerase inhibitors against key veterinary pathogens. [Abstract]

2023 Sep:284:109840. PMID: 37531840
bioRxiv

2026 Feb 23.
University of Szeged

2019 Jan.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- 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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Farrell DJ, et al. In Vitro Activity of Gepotidacin (GSK2140944) against Neisseria gonorrhoeae. Antimicrob Agents Chemother. 2017 Feb 23;61(3). [Content Brief]

[2]. Biedenbach DJ, et al. In Vitro Activity of Gepotidacin, a Novel Triazaacenaphthylene Bacterial Topoisomerase Inhibitor, against a Broad Spectrum of Bacterial Pathogens. Antimicrob Agents Chemother. 2016 Jan 4;60(3):1918-23. [Content Brief]

[3]. O'Riordan W, et al. Efficacy, Safety, and Tolerability of Gepotidacin (GSK2140944) in the Treatment of Patients with Suspected or Confirmed Gram-Positive Acute Bacterial Skin and Skin Structure Infections. Antimicrob Agents Chemother. 2017 May 24;61(6). [Content Brief]

[4]. So W, et al. Pharmacodynamic Profile of GSK2140944 against Methicillin-Resistant Staphylococcus aureus in a Murine Lung Infection Model. Antimicrob Agents Chemother. 2015 Aug;59(8):4956-61. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

Gepotidacin

12 Cited Publications

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Gepotidacin

Publications Citing Use of MedChemExpress (MCE) Gepotidacin

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Alle Topoisomerase Isoform-spezifische Produkte anzeigen