| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Trovafloxacin mesylate 是一种有效的特异性 pannexin 1 通道抑制剂 (PANX1, IC50 = 4 μM)。Trovafloxacin mesylate 对革兰氏阳性、革兰氏阴性和厌氧菌具有强效活性。 Trovafloxacin mesylate 阻断 DNA 促旋酶和拓扑异构酶 IV 活性。
产品描述 | Trovafloxacin mesylate is an effective and selective inhibitor of pannexin 1 channel (PANX1, IC50 = 4 μM). Trovafloxacin mesylate exhibits potent activity against Gram-positive, Gram-negative, and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. |
靶点活性 | Pannexin 1 channel (PANX1):4 μM |
体外活性 | Trovafloxacin mesylate is an inhibitor of TO-PRO-3 uptake by apoptotic cells and inhibits ATP release from apoptotic cells. Trovafloxacin mesylate does not inhibit caspase 3/7 activation, or caspase-mediated PANX1 cleavage during apoptosis[1]. Trovafloxacin mesylate is equally active against both penicillin-susceptible and -resistant pneumococci, with MICs of 0.06-0.25 mg/mL reported for more than 700 isolates. The MICs of Trovafloxacin mesylate at which 90% of isolates are inhibited for 55 isolates of pneumococci is 0.125 μg/mL[2]. Trovafloxacin mesylate prolongs TNF-induced activation of MAPKs and IKKα/β activation in HepG2 cells. Trovafloxacin mesylate (20 µM; 24 hours) and tumor necrosis factor (TNF; 4 ng/mL) incubation induces apoptosis and increases leakage of lactate dehydrogenase (LDH). Trovafloxacin mesylate (20 µM; 24 hours) and TNF (4 ng/mL) incubation increases expression of early NF-κB-related factors A20 and IκBα[3]. |
体内活性 | Trovafloxacin mesylate induces severe liver toxicity associated with vast apoptotic areas in the liver, increased serum levels of alanine amino transferases (ALT) and pro-inflammatory cytokines when administered in combination with lipopolysaccharide (LPS |
分子量 | 512.46 |
分子式 | C21H19F3N4O6S |
CAS No. | 147059-75-4 |
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 120 mg/mL (234.16 mM), ultrasonic and warming and heat to 60°C
H2O: 18 mg/mL (35.12 mM), Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Trovafloxacin mesylate 147059-75-4 Cell Cycle/Checkpoint DNA Damage/DNA Repair Microbiology/Virology Others Antibacterial DNA/RNA Synthesis Topoisomerase topoisomerase-IV TNF gyrase Bacterial hepatotoxicity LPS Trovafloxacin broad-spectrum Antibiotic DNA Inhibitor PANX1 pneumococci inhibit pro-inflammatory NF-κB inhibitor