1-Ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic Acid Sesquihydrate; Enoxacin; Penetrex|r The Clorox Company; Bactidan
应用
A quinolone antibacterial agent that acts on DNA gyrase.
规格或纯度
≥98%
运输条件
常规运输
生化机理
Enoxacin is a quinolone antibacteral agent. Acts on DNA gyrase.
一般描述
Enoxacin 是一种口服的广谱喹诺酮类抗菌剂,用于治疗尿路感染和淋病。常见的副作用有失眠。A quinolone antibacterial agent that acts on DNA gyrase.
Enoxacin is an oral broad-spectrum fluoroquinolone antibacterial agent used in the treatment of urinary tract infections and gonorrhea. Insomnia is a common adverse effect. A quinolone antibacterial agent that acts on DNA gyrase.
相关属性
CAS编号
84294-96-2
敏感性
对光线敏感,易吸潮
熔点
225.0 – 229.0 °C
溶解性
Soluble in water (Partly), 1 M NaOH (50 mg/ml, Yellow, Clear to Slightly Hazy), DMSO (Sparingly), chloroform (Sparingly), and methanol (Sparingly).
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 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.
[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.
L-α-Methyl-DOPA · sesquihydrate is a DDC (L-Aromatic amino acid decarboxylase) inhibitor. Adrenergic inhibiting agent used for antihypertensive treatment.
规格或纯度
≥98%
运输条件
冰袋运输
生化机理
L-α-Methyl-DOPA · sesquihydrate is a DDC (L-Aromatic amino acid decarboxylase) inhibitor. Adrenergic inhibiting agent used for antihypertensive treatment.α2 adrenoceptor agonist. Competitive DOPA decarboxylase inhibitor. Centrally and peripherally acting. Depletes tissue levels of norepinephrine. Shows antihypertensive effects in vivo. Orally active.
一般描述
Methyldopa 是DOPA 脱羧酶竞争性抑制剂,ED50为21.8 mg/kg。L-α-Methyl-DOPA · sesquihydrate is a DDC (L-Aromatic amino acid decarboxylase) inhibitor. Adrenergic inhibiting agent used for antihypertensive treatment.
Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg. L-α-Methyl-DOPA · sesquihydrate is a DDC (L-Aromatic amino acid decarboxylase) inhibitor. Adrenergic inhibiting agent used for antihypertensive treatment.
相关属性
CAS编号
41372-08-1
敏感性
对光和空气敏感
熔点
>300°C
溶解性
Soluble in water (sparingly), 0.1M HCl (5 %, clear, colorless to faint yellow solution), and dilute mineral acids. Almost insoluble in common organic solvents.
L-α-Methyl-DOPA · sesquihydrate is a DDC (L-Aromatic amino acid decarboxylase) inhibitor. Adrenergic inhibiting agent used for antihypertensive treatment.α2 adrenoceptor agonist. Competitive DOPA decarboxylase inhibitor. Centrally and peripherally acting. Depletes tissue levels of norepinephrine. Shows antihypertensive effects in vivo. Orally active.
一般描述
Methyldopa 是DOPA 脱羧酶竞争性抑制剂,ED50为21.8 mg/kg。
Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg. L-α-Methyl-DOPA · sesquihydrate is a DDC (L-Aromatic amino acid decarboxylase) inhibitor. Adrenergic inhibiting agent used for antihypertensive treatment.