1. Anti-infection
  2. Bacterial

Gepotidacin (Synonyms: GSK2140944)

Cat. No.: HY-16742 Purity: 99.26% ee.: 100.00%
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 USD 414 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 720 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 2340 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 3360 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Gepotidacin:

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  • 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
Solvent & Solubility
In Vitro: 

10 mM in 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
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

448.52

Formula

C₂₄H₂₈N₆O₃

CAS No.

1075236-89-3

SMILES

O=C(C=NC(C=C1)=C23)N3[[email protected]](CN4CCC(NCC5=CC(CCCO6)=C6C=N5)CC4)CN2C1=O

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

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

Cat. No.: HY-16742