S29883 |
Trovafloxacin |
源葉(MedMol) | 98% |
Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.402 ml | 12.009 ml | 24.018 ml |
5 mM | 0.48 ml | 2.402 ml | 4.804 ml |
10 mM | 0.24 ml | 1.201 ml | 2.402 ml |
50 mM | 0.048 ml | 0.24 ml | 0.48 ml |
- 產品描述:
Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1
- 靶點: Quinolone;DNAgyrase;Topoisomerase;Antibacterial;Antibiotic
- 體內研究:
Trovafloxacin (150 mg/kg; oral administration; male C57BL/6 J mice) treatment disrupts TNF-induced p65 nuclear translocation. Trovafloxacin treatment increases expression of early NF-κB-related factors A20 and IκBα. Trovafloxacin, when administered in combination with lipopolysaccharide (LPS) or TNF to mice induces severe liver toxicity associated with vast apoptotic areas in the liver, increased serum levels of alanine amino transferases (ALT) and pro-inflammatory cytokines.
- 參考文獻:
1. 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. 2. Poon IK, et al. Unexpected link between an antibiotic, pannexin channels and apoptosis. Nature. 2014 Mar 20;507(7492):329-34. 3. 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.
- 溶解性: DMSO : 10 mg/mL (24.02 mM; ultrasonic and adjust pH to 4 with HCl)
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 2.402 ml 12.009 ml 24.018 ml 5 mM 0.48 ml 2.402 ml 4.804 ml 10 mM 0.24 ml 1.201 ml 2.402 ml 50 mM 0.048 ml 0.24 ml 0.48 ml
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質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)