Enoxacin hydrate(Synonyms: 依诺沙星倍半水合物; Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate)

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Enoxacin hydrate (Synonyms: 依诺沙星倍半水合物; Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate) 纯度: 98.15%

Enoxacin hydrate (Enoxacin sesquihydrate) 是一种氟喹诺酮，可以干扰 DNA 复制，抑制细菌 DNA 促旋酶 (IC50=126 µg/ml) 和拓扑异构酶 IV (IC50=26.5 µg/ml)。Enoxacin hydrate 是一种 miRNA 加工激活剂，可增强 siRNA 介导的 mRNA 降解并促进内源性 miRNA 的生物发生，也可增强 TAR RNA 结合蛋白 2 (TRBP) 介导的 microRNA 加工。Enoxacin hydrate 有效抑制革兰氏阳性和阴性细菌， 是一种特异性的癌症生长抑制剂。

Enoxacin hydrate(Synonyms: 依诺沙星倍半水合物; Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate)

Enoxacin hydrate Chemical Structure

CAS No. : 84294-96-2

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生物活性

Enoxacin hydrate (Enoxacin sesquihydrate), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin hydrate is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin hydrate has potent activities against gram-positive and -negative bacteria. Enoxacin hydrate is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing[1][2][3][4].

体外研究
(In Vitro)

Enoxacin hydrate (Enoxacin sesquihydrate) increases siGFP-mediated gene knockdown mediated by siRNA against EGFP in HEK293 cells-based reporter system in a dose-dependent manner, with a median effective concentration (EC50) of ~30 µM, whereas it has no effect on the cells expressing GFP only. Enoxacin (50 µM) promotes the processing of miRNAs and the loading of siRNA duplexes onto RISCs in HEK293 cells[3].
Enoxacin has no effect on the processing of pre-let-7 or pre-miR-30a by Dicer alone. However, the addition of Enoxacin can enhance the processing of let-7 or pre-miR-30a by Dicer and TRBP together[3].
Enoxacin inhibits 90% Escherichia coli, Klebsiella sp., Aeromonas sp., Enterobacter spp., Serratia spp., Proteus mirabilis, and Morganella morganii at less than or equal to 0.8 micrograms/ml[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Enoxacin hydrate (Enoxacin sesquihydrate; 100 µM; 2 µl; injected into ear once a day for 3 consecutive days (days 12, 13 and 14)) enhances the the GFP mRNA knockdown efficiency by Lv-siGFP (from 80% to 60%; 40% GFP mRNA level remained), whereas alone has no effect on GFP expression in GFP transgenic line C57BL/6-Tg(ACTB-EGFP)1Osb/J (10 d old) with lentivirus expressing shGFP (Lv-siGFP; injected into ear for 10 days)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

347.34

Formula

C15H20FN4O4.5
CAS 号

84294-96-2
中文名称

依诺沙星倍半水合物
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

1M NaOH : 100 mg/mL (287.90 mM; ultrasonic and adjust pH to 11 with NaOH)

DMSO : 2.78 mg/mL (8.00 mM; Need ultrasonic)

H2O : 1 mg/mL (2.88 mM; ultrasonic and warming and heat to 80°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8790 mL 14.3951 mL 28.7902 mL
5 mM 0.5758 mL 2.8790 mL 5.7580 mL
10 mM 0.2879 mL 1.4395 mL 2.8790 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Sonia Melo, et al.Small molecule enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2-mediated microRNA processing. Proc Natl Acad Sci U S A. 2011 Mar 15;108(11):4394-9.

    [2]. M Takei, et al. Target preference of 15 quinolones against Staphylococcus aureus, based on antibacterial activities and target inhibition. Antimicrob Agents Chemother. 2001 Dec;45(12):3544-7.

    [3]. Ge Shan, et al. A small molecule enhances RNA interference and promotes microRNA processing. Nat Biotechnol. 2008 Aug;26(8):933-40.

    [4]. Rengen Fan, et al. Small molecules with big roles in microRNA chemical biology and microRNA-targeted therapeutics. RNA Biol. 2019 Jun;16(6):707-718.

    [5]. Chin, N.-X. and H.C. Neu, In vitro activity of enoxacin, a quinolone carboxylic acid, compared with those of norfloxacin, new beta-lactams, aminoglycosides, and trimethoprim. Antimicrobial agents and chemotherapy, 1983. 24(5): p. 754-763.

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