Trovafloxacin-d4 mesylate(Synonyms: 曲伐沙星甲磺酸盐 d4 (甲磺酸盐))

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物，专注于信号通路和疾病研究领域。
Trovafloxacin-d4 mesylate (Synonyms: 曲伐沙星甲磺酸盐 d4 (甲磺酸盐))

Trovafloxacin-d4 mesylate 是 Trovafloxacin mesylate 的氘代物。Trovafloxacin mesylate 是一种广谱喹诺酮类抗生素，对革兰氏阳性，革兰氏阴性和厌氧菌具有有效的活性。Trovafloxacin mesylate 可阻断 DNA 促旋酶 (DNA gyrase) 和拓扑异构酶 IV (topoisomerase IV) 的活性。Trovafloxacin mesylate 也是一种有效的，选择性的，口服活性的 Pannexin 1 通道 (PANX1) 抑制剂，对 PANX1 内向电流的 IC50 为 4 μM。Trovafloxacin mesylate 不抑制连接蛋白 43 间隙连接或 PANX2。Trovafloxacin mesylate 通过抑制 PANX1 导致凋亡细胞碎片失调。

Trovafloxacin-d4 mesylate(Synonyms: 曲伐沙星甲磺酸盐 d4 (甲磺酸盐))

Trovafloxacin-d4 mesylate Chemical Structure

CAS No. : 1346601-60-2

规格 是否有货
1 mg Check price and availability
10 mg Check price and availability

* Please select Quantity before adding items.

生物活性

Trovafloxacin-d4 mesylate is the deuterium labeled Trovafloxacin mesylate. Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

516.48

Formula

C21H15D4F3N4O6S
CAS 号

1346601-60-2
中文名称

曲伐沙星甲磺酸盐 d4 (甲磺酸盐)
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Giustarini G, et al. The hepatotoxic fluoroquinolone trovafloxacin disturbs TNF- and LPS-induced p65 nuclear translocation in vivo and in vitro. Toxicol Appl Pharmacol. 2020 Mar 15;391:114915.

    [3]. Poon IK, et al. Unexpected link between an antibiotic, pannexin channels and apoptosis. Nature. 2014 Mar 20;507(7492):329-34.

    [4]. Gootz TD, et al. Activity of the new fluoroquinolone trovafloxacin (CP-99,219) against DNA gyrase and topoisomerase IV mutants of Streptococcus pneumoniae selected in vitro. Antimicrob Agents Chemother. 1996 Dec;40(12):2691-7.

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