货号	规格	价格	上海	北京	珠海	重庆	武汉
S81890-1mg买3赠1	98.56%	￥1100.00 ￥880.00 S81890-1mg ￥880.00 现货（买3赠1）	3 3	-	-	-	-
S81890-5mg买3赠1	98.56%	￥3320.00 ￥2650.00 S81890-5mg ￥2650.00 现货（买3赠1）	7 7	-	-	-	-
S81890-10mg促销	98.56%	￥6000.00 ￥4800.00 S81890-10mg ￥4800.00 现货	5 5	-	-	-	-
S81890-25mg促销	98.56%	￥12000.00 ￥9600.00 S81890-25mg ￥9600.00 现货	4 4	-	-	-	-

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产品描述：

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

靶点：

Bacterial;Topoisomerase;Others

体外研究：

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)

体内研究：

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.

参考文献：

1. Farrell DJ, et al. In Vitro Activity of Gepotidacin (GSK2140944) against Neisseria gonorrhoeae. Antimicrob Agents Chemother. 2017 Feb 23;61(3). 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. 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). 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.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.23 ml	11.148 ml	22.296 ml
5 mM	0.446 ml	2.23 ml	4.459 ml
10 mM	0.223 ml	1.115 ml	2.23 ml
50 mM	0.045 ml	0.223 ml	0.446 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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