Home Tools

Cart

Gepotidacin

Catalog No. T11391L CAS 1075236-89-3

Synonyms: GSK2140944

Gepotidacin is a novel triazaacenaphthylene inhibitor of bacterial type II topoisomerase.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Gepotidacin, CAS 1075236-89-3

Pack Size	Availability	Price/USD
5 mg	10-14 weeks	$ 364.00
25 mg	10-14 weeks	$ 1,490.00
50 mg	10-14 weeks	$ 1,940.00
100 mg	10-14 weeks	$ 2,780.00

Bulk Inquiry

This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Gepotidacin is a novel triazaacenaphthylene inhibitor of bacterial type II topoisomerase.
In vitro	Gepotidacin has in vitro activity against causative pathogens of acute bacterial skin and skin structure infections (ABSSSIs) [3]. Gepotidacin 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 isolate tested are 0.12 and 0.25 μg/mL, respectively [1]. The gepotidacin MIC90s are as follows: Streptococcus pyogenes (0.25 μg/mL); Escherichia coli (2 μg/mL); Moraxella catarrhalis (≤0.06 μg/mL); Streptococcus pneumoniae (0.25 μg/mL); Haemophilus influenzae (1 μg/mL); Clostridium perfringens (0.5 μg/mL); and Shigella spp. (1 μg/mL) [2].
In vivo	ELF penetration ratios vary between 1.1 and 1.4. GSK2140944 exhibits minimum inhibitory concentrations (MICs) of 0.125 to 0.5 mg/L against six MRSA isolates. The average area under the curve (AUC)/MIC ratios necessary for bacterial stasis and a decrease of 1 log-unit are 59.3 ± 34.6 and 148.4 ± 83.3, respectively. The maximal reductions observed amount to 1.1 to 3.1 log10 CFU in neutropenic mice [4].

Synonyms	GSK2140944
Molecular Weight	448.52
Formula	C24H28N6O3
CAS No.	1075236-89-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 7.14 mg/mL (15.92 mM), Sonication is recommended.

References and Literature

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

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Gepotidacin 1075236-89-3 Others GSK2140944 GSK 2140944 GSK-2140944 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.