GSK-2140944

Research use only, not for human use.

GSK-2140944 (Gepotidacin) is a novel potent, selective bacterial type II topoisomerase inhibitor in development for the treatment of conventional and biothreat pathogens.

GSK-2140944 (Gepotidacin) is a novel potent, selective bacterial type II topoisomerase inhibitor in development for the treatment of conventional and biothreat pathogens, including Gram-positive pathogens and MRSA; shows antibacterial activity against MSSA and MRSA isolates (MIC90=0.5 ug/ml).Bacterial Infection Phase 2 Clinical.

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. 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., Gepotidacin hasin vitroactivity against causative pathogens of acute bacterial skin and skin structure infections (ABSSSIs).

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.

Gepotidacin | GSK2140944

GPCR/G Protein

Antibacterial

Antibacterial

Infection

Bacterial Infection

1075236-89-3

448.527

C24H28N6O3

>98% (HPLC)

DMSO : 7.14 mg/mL 15.92 mM

O=C(C=NC(C=C1)=C23)N3[C@H](CN4CCC(NCC(N=C5)=CC6=C5OCCC6)CC4)CN2C1=O

(2R)-2-[[4-[[(3,4-Dihydro-2H-pyrano[2,3-c]pyridin-6-yl)methyl]amino]-1-piperidinyl]methyl]-1,2-dihydro-3H,8H-2a,5,8a-triazaacenaphthylene-3,8-dione

(-20℃)

With Ice Pack

≥ 2 years