1. Anti-infection
  2. Bacterial

Gepotidacin (Synonyms: GSK2140944)

Cat. No.: HY-16742 Purity: 99.26% ee.: 100.00%
Data Sheet SDS Handling Instructions

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

For research use only. We do not sell to patients.
Gepotidacin Chemical Structure

Gepotidacin Chemical Structure

CAS No. : 1075236-89-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO $345 In-stock
1 mg $110 In-stock
5 mg $350 In-stock
10 mg $600 In-stock
50 mg $1950 In-stock
100 mg $2800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Gepotidacin:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

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].

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.

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume 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
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[4]

Gepotidacin is prepared in normal saline.

Mouse: 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
Molecular Weight

448.52

Formula

C₂₄H₂₈N₆O₃

CAS No.

1075236-89-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Gepotidacin
Cat. No.:
HY-16742
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