Gepotidacin (Synonyms: GSK2140944)

Name: Gepotidacin
Brand: MedChemExpress
SKU: HY-16742
Rating: 5.0 (12 reviews)

Cat. No.: HY-16742 Purity: 99.92%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 1075236-89-3

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
1 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

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

고객리뷰

Based on 12 publication(s) in Google Scholar

Other Forms of Gepotidacin:

12 Publications Citing Use of MCE Gepotidacin

Gel Electrophoresis

Microbiological Assay

: 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-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.

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Topoisomerase Topo I Topo II DNA gyrase

Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

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.

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

분자량

448.52

화학식

C₂₄H₂₈N₆O₃

CAS No.

1075236-89-3

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

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

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
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.

몰농도 계산기
농도 희석 계산기

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
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

mg/kg

Animal weight
(per animal)

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.

순도&문서

Purity: 99.92%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

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

Handling Instructions (2659 KB)

References

[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]

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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.

References

[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]

Complete Stock Solution Preparation Table

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

Gepotidacin Related Classifications

Infection

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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Gepotidacin (Synonyms: GSK2140944)

고객리뷰

Other Forms of Gepotidacin:

Gepotidacin Related Antibodies

12 Publications Citing Use of MCE Gepotidacin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Antibiotic Isoform Specific Products:

View All Topoisomerase Isoform Specific Products:

Biological Activity

Protocol

순도&문서

References

고객리뷰

Gepotidacin Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Gepotidacin Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report