Gepotidacin

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Gepotidacin

CAS No. : 1075236-89-3

MCE 国际站：Gepotidacin

产品活性：Gepotidacin (GSK2140944)是一种新型的三氮杂苊烯细菌II型拓扑异构酶抑制剂。

研究领域：Anti-infection  |  Cell Cycle/DNA Damage

作用靶点：Bacterial  |  Topoisomerase

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

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.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Anti-Infection Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Antibacterial Compound Library  |  Anti-COVID-19 Compound Library  |  Anti-Lung Cancer Compound Library  |  Heterocyclic Compound Library  |  Rapamycin  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Dexamethasone  |  Puromycin dihydrochloride  |  Dimethyl sulfoxide  |  Staurosporine  |  Actinomycin D  |  G-418 disulfate  |  Etoposide  |  5-Azacytidine  |  Nigericin sodium salt  |  Brefeldin A  |  Estradiol  |  CCCP  |  Ionomycin  |  Resveratrol  |  Hygromycin B  |  Tunicamycin  |  Exatecan mesylate  |  Mitomycin C  |  Everolimus  |  Doxycycline hyclate  |  Tacrolimus  |  Methotrexate  |  SN-38  |  Neomycin sulfate  |  Acetaminophen

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds