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147059-75-4

中文名稱 曲伐沙星甲磺酸鹽
英文名稱 Trovafloxacin Mesylate
CAS 147059-75-4
分子式 C21H19F3N4O6S
分子量 512.46
MOL 文件 147059-75-4.mol
更新日期 2026/07/16 08:22:01
147059-75-4 結(jié)構(gòu)式 147059-75-4 結(jié)構(gòu)式

基本信息

中文別名
曲伐沙星甲磺酸
曲伐沙星甲磺酸鹽
英文別名
Trovan
CP 99219-27
Unii-0p1lko80wn
Trovafloxacin MonoMeth
Trovafloxacin Methanesulfonate
Trovafloxacin monomethanesulfonate
Trovafloxacin mesylate - CP 99219 mesylate
7-[(1S,5R)-6-amino-3-azabicyclo[3.1.0]hex-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid
7-[(1α,5α,6α)-6-Amino-3-azabicyclo[3.1.0]hex-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylicacidmesylate
(1α,5α,6α)-7-(6-Amino-3-azabicyclo[3.1.0]hex-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid methanesulfonate

物理化學(xué)性質(zhì)

熔點>250°C (dec.)
儲存條件room temp
溶解度二甲基亞砜:>10mg/mL
形態(tài)粉末
顏色白色至灰白色
InChIKeyDYNZICQDCVYXFW-AHZSKCOENA-N
SMILESS(O)(=O)(=O)C.O=C1C(=CN(C2C=CC(F)=CC=2F)C2=NC(N3C[C@@]4([H])[C@H](N)[C@@]4([H])C3)=C(F)C=C12)C(=O)O |&1:23,25,27,r|

安全數(shù)據(jù)

危險性符號(GHS)腐蝕 (GHS05)健康危害 (GHS08)
GHS05,GHS08
警示詞危險
危險性描述H314-H361
危險品標志C
危險類別碼63-34
安全說明26-36-45
危險品運輸編號UN 1759 8 / PGIII
WGK Germany3
RTECS號QN2791250
存儲類別8A - Combustible corrosive hazardous materials
危險性類別Repr. 2
Skin Corr. 1B
毒性women,LDLo,oral,2mg/kg (2mg/kg),SKIN AND APPENDAGES (SKIN): "DERMATITIS, OTHER: AFTER SYSTEMIC EXPOSURE",Archives of Internal Medicine. Vol. 159, Pg. 2225, 1999.
曲伐沙星甲磺酸鹽價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2026/06/05HY-103399曲伐沙星甲磺酸鹽
Trovafloxacin mesylate
147059-75-45 mg900元
2026/06/05HY-103399曲伐沙星甲磺酸鹽
Trovafloxacin mesylate
147059-75-410 mM * 1 mL in DMSO1015元
2026/06/05HY-103399曲伐沙星甲磺酸鹽
Trovafloxacin mesylate
147059-75-410 mg1500元

常見問題列表

生物活性
Trovafloxacin mesylate 是一種廣譜喹諾酮類抗生素,對革蘭氏陽性,革蘭氏陰性和厭氧菌具有有效的活性。Trovafloxacin mesylate 可阻斷 DNA 促旋酶 (DNA gyrase) 和拓撲異構(gòu)酶 IV (topoisomerase IV) 的活性。Trovafloxacin mesylate 也是一種有效的,選擇性的,口服活性的 Pannexin 1 通道 (PANX1) 抑制劑,對 PANX1 內(nèi)向電流的 IC50 為 4 μM。Trovafloxacin mesylate 不抑制連接蛋白 43 間隙連接或 PANX2。Trovafloxacin mesylate 通過抑制 PANX1 導(dǎo)致凋亡細胞碎片失調(diào)。
靶點

IC50: 4 μM (Pannexin 1 channel (PANX1))
Gram-positive, Gram-negative and anaerobic organisms
DNA gyrase
Topoisomerase IV

體外研究

Trovafloxacin (20 μM; 24 hours; HepG2 cells) and tumor necrosis factor (TNF; 4 ng/mL) incubation induces apoptosis and increases leakage of lactate dehydrogenase (LDH) in HepG2 cells.
Trovafloxacin (20 μM; 24 hours; HepG2 cells) and TNF (4 ng/mL) incubation increases expression of early NF-κB-related factors A20 and IκBα.
Trovafloxacin prolongs TNF-induced activation of MAPKs and IKKα/β activation in HepG2.
Trovafloxacin is a potent inhibitor of TO-PRO-3 uptake by apoptotic cells. Trovafloxacin also inhibits ATP release from apoptotic cells. Trovafloxacin does not inhibit caspase 3/7 activation, or caspase-mediated PANX1 cleavage during apoptosis.
Trovafloxacin 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 at which 90% of isolates are inhibited for 55 isolates of pneumococci is 0.125 μg/mL.

Apoptosis Analysis

Cell Line: HepG2 cells
Concentration: 20 μM
Incubation Time: 24 hours
Result: Showed a gradual increase of Annexin V-staining and an increased leakage of lactate dehydrogenase (LDH) at 24 h.

RT-PCR

Cell Line: HepG2 cells
Concentration: 20 μM
Incubation Time: 24 hours
Result: Caused a higher increase in the transcription of A20 and IκBα in HepG2 cells.
體內(nèi)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.

Animal Model: Male C57BL/6 J mice (9-11-week-old) injected with recombinant murine TNF ion
Dosage: 150 mg/kg
Administration: Oral administration; once
Result: Showed a greater number of cells with increased nuclear/cytoplasmic p65 ratio in liver.
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