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147059-72-1

中文名稱 曲伐沙星
英文名稱 TROVAFLOXACIN
CAS 147059-72-1
分子式 C20H15F3N4O3
分子量 416.35
MOL 文件 147059-72-1.mol
更新日期 2024/05/20 09:19:54
147059-72-1 結(jié)構(gòu)式 147059-72-1 結(jié)構(gòu)式

基本信息

中文別名
特伐沙星
曲伐沙星
曲氟沙星
聚苯乙烯磺酸鈣
曲伐沙星,曲氟沙星
(1Α,5Α,6Α)-7-(6-氨基-3-氮雜二環(huán)[3.1.0]己-3-基)-1-(2,4-二氟苯基)-6-氟-1,4-二氫-4-氧-1,8-萘啶-3-羧酸
英文別名
CP-99219
TROVAFLOXACIN
Trovan:CP-99219-27
7-[(1R,5S)-6-amino-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid
7-[(1R,5S)-6-azanyl-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid
7-[(1R,5S)-6-amino-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-keto-1,8-naphthyridine-3-carboxylic acid
(1α,5α,6α)-7-(6-Amino-3-azabi-cyclo[3.1.0]hex-3-y1)-1-(2,4-difluomphenyl)-6-fluom-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid
1,8-Naphthyridine-3-carboxylic acid, 7-(1.alpha.,5.alpha.,6.alpha.)-6-amino-3-azabicyclo3.1.0hex-3-yl-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-
所屬類別
藥物: 抗病源性微生物藥: 喹諾酮類藥物

物理化學(xué)性質(zhì)

外觀性狀鹽酸特伐沙星(Trovafloxacin Hydrochloride):C20H15F3N4O3?HCl。 [146961-34-4]。從乙腈-甲醇得淡黃色結(jié)晶,熔點(diǎn)246℃(分解)。
熔點(diǎn)>195oC (dec.)
沸點(diǎn)630.5±55.0 °C(Predicted)
密度1.612±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C Freezer, Under inert atmosphere
溶解度可溶于乙腈(少許)、DMSO(少許)
酸度系數(shù)(pKa)5.80±0.70(Predicted)
形態(tài)固體
顏色淡米色至淺米色
CAS 數(shù)據(jù)庫147059-72-1

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335

應(yīng)用領(lǐng)域

用途1
喹諾酮類抗菌藥。

制備方法

方法1
450ml THF、50ml水、127ml甲磺酸和7-氯-1-(2,4-二氟苯基)-7-氟-1,4-二氫-4-氧代-1,8-喹啉-3-羧酸乙酯一起回流1h,冷至25℃。過濾收集結(jié)晶,用THF洗,真空干燥,得7-氯-1-(2,4-二氟苯基)-7-氟-1,4-二氫-4-氧代-1,8-喹啉-3-羧酸,收率89%,mp 250℃。
500mg 7-氯-1-(2,4-二氟苯基)-7-氟-1,4-二氫-4-氧代-1,8-喹啉-3-羧酸、624mg(1α,5α,6α)-6-氨基-3-氮雜二環(huán)[3.1.0]己烷二甲苯磺酸鹽、0.6ml三乙胺和5ml甲醇,一起回流16h。過濾收集形成的白色固體,在THF中回流,再過濾收集。得450ml特伐沙星,收率75%,mp 225~228℃(分解)。

常見問題列表

生物活性
Trovafloxacin 是一種廣譜喹諾酮類抗生素,對(duì)革蘭氏陽性,革蘭氏陰性和厭氧菌具有有效的活性。Trovafloxacin 可阻斷 DNA 促旋酶 (DNA gyrase) 和拓?fù)洚悩?gòu)酶 IV (topoisomerase IV) 的活性。Trovafloxacin 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(duì) PANX1 內(nèi)向電流的 IC50 為 4 μM。Trovafloxacin 不抑制 connexin 43 gap junction 或 PANX2。Trovafloxacin 通過抑制 PANX1 導(dǎo)致凋亡細(xì)胞碎片失調(diào)。
靶點(diǎn)

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
Result: Showed a greater number of cells with increased nuclear/cytoplasmic p65 ratio in liver.
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