プルリフロキサシン
プルリフロキサシン 物理性質
- 融点 :
- 211-214°C
- 沸点 :
- 633.2±65.0 °C(Predicted)
- 比重(密度) :
- 1.62±0.1 g/cm3(Predicted)
- 貯蔵温度 :
- Sealed in dry,Store in freezer, under -20°C
- 溶解性:
- 1M NaOH:25MLに可溶、無色透明(溶媒:1mg+25mL NaOH)
- 酸解離定数(Pka):
- 5.85±0.40(Predicted)
- 外見 :
- 白色から黄色の結晶性固体。
- 色:
- オフホワイトからペールイエロー
- 極大吸収波長 (λmax):
- 276nm(H2O)(lit.)
- Merck :
- 14,7908
- CAS データベース:
- 123447-62-1(CAS DataBase Reference)
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
RTECS 番号 |
XJ0600000 |
|
|
HSコード |
2941.90.3000 |
|
|
絵表示(GHS) |
|
注意喚起語 |
警告 |
危険有害性情報 |
コード |
危険有害性情報 |
危険有害性クラス |
区分 |
注意喚起語 |
シンボル |
P コード |
H302 |
飲み込むと有害 |
急性毒性、経口 |
4 |
警告 |
|
P264, P270, P301+P312, P330, P501 |
H315 |
皮膚刺激 |
皮膚腐食性/刺激性 |
2 |
警告 |
|
P264, P280, P302+P352, P321,P332+P313, P362 |
H319 |
強い眼刺激 |
眼に対する重篤な損傷性/眼刺激 性 |
2A |
警告 |
|
P264, P280, P305+P351+P338,P337+P313P |
H335 |
呼吸器への刺激のおそれ |
特定標的臓器毒性、単回暴露; 気道刺激性 |
3 |
警告 |
|
|
|
注意書き |
P261 |
粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。 |
P305+P351+P338 |
眼に入った場合:水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。 |
|
プルリフロキサシン 価格
もっと(9)
メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
富士フイルム和光純薬株式会社(wako)
|
W01LKTP7082 |
プルリフロキサシン
Prulifloxacin |
123447-62-1 |
25mg |
¥9800 |
2024-03-01 |
購入 |
富士フイルム和光純薬株式会社(wako)
|
W01LKTP7082 |
プルリフロキサシン
Prulifloxacin |
123447-62-1 |
100mg |
¥15800 |
2024-03-01 |
購入 |
東京化成工業
|
P2058 |
プルリフロキサシン >98.0%(HPLC)(T)
Prulifloxacin
>98.0%(HPLC)(T) |
123447-62-1 |
1g |
¥15500 |
2024-03-01 |
購入 |
東京化成工業
|
P2058 |
プルリフロキサシン >98.0%(HPLC)(T)
Prulifloxacin
>98.0%(HPLC)(T) |
123447-62-1 |
5g |
¥53500 |
2024-03-01 |
購入 |
Sigma-Aldrich Japan
|
SML3707 |
≥98% (HPLC)
Prulifloxacin ≥98% (HPLC) |
123447-62-1 |
10MG |
¥8400 |
2023-06-01 |
購入 |
プルリフロキサシン 化学特性,用途語,生産方法
外観
うすい黄赤色~黄色~緑色粉末~結晶
用途
キノロン系抗菌薬
効能
抗菌薬, 核酸合成阻害薬
商品名
スオード (Meiji Seikaファルマ)
説明
Prulifloxacin was launched as the third fluoroquinone. It was introduced in
Japan as an oral treatment for urinary tract infections (UTls), respiratory tract infections
(RTls) and bacterial pneumoniae. It can be synthesized in 10 steps from commercially
available 3,4-difluoroaniline. Key steps involve the cyclization of 6,7-difluoro-rl-hydroxy-2-
thioquinoline-3carboxylic acid ethyl ester with 1 ,I-dibromomethane to give the
corresponding thiazeto-[3,2a]quinoline. Aromatic nucleophilic substitution of the 7-fluoro
atom with piperazine followed by hydrolysis of the ethyl ester and finally alkylation of the
piperazinyl moiety with 4-(bromomethyl)-5-methyl-l ,bdioxol-Bone complete the synthesis.
Prulifloxacin is a lipophilic prodrug, which is rapidly hydrolyzed to the corresponding Ndealkylated
piperazine, NM 394, by paraoxonase type enzymes in blood and liver following
intestinal absorption. The DNA gyrase inhibitor NM 394 accounts for all antimicrobial
activity: it shows a similar or greater activity against gram-positive bacteria compared to
ciprofloxacin, and a greater activity in the case of gram-negative bacteria. In clinical
studies, prulifloxacin has shown good efficacy against UTls and RTls. The drug is mainly
excreted in the urine and in the feces as unchanged NM 394, which has a plasma half-life
of approximately 8 h. Phototoxicity in animal models is less severe than with other
quinolones. Prulifloxacin is well tolerated with an adverse effect profile similar to that of
other fluoroquinolones.
化学的特性
Off-White Solid
使用
Prulifloxacin is a synthetic chemotherapeutic antibiotic of the fluoroquinolone drug class. Prulifloxacin is a prodrug for active metabolite, Ulifloxacin. Antibacterial.
応用例(製薬)
A lipophilic prodrug which is very rapidly metabolized by esterase into ulifloxacin, a 6-fluoro, 7-piperazinyl thiazetoquinoline.
Ulifloxacin is moderately active against Staph. aureus (MIC 0.4–0.8 mg/L) and inactive against Str. pneumoniae (MIC 2–8 mg/L) as well as against Enterococcus spp. Against Enterobacteriaceae (MIC 0.05–0.8 mg/L) and Ps. aeruginosa (MIC 0.2–0.8 mg/L) activity is similar to that of ciprofloxacin. It is active against fastidious Gram-negative bacilli, but not against anaerobes and non-fermentative Gram-negative bacilli. Activity against Acinetobacter spp. is modest.
Prulifloxacin is rapidly converted into ulifloxacin and after 3 h is no longer detected in blood. In volunteers receiving a single oral dose, peak plasma concentrations of 0.68 mg/L (300 mg dose) to 1.88 mg/L (for 400 mg dose) were attained between 0.67 and 1.25 h. The mean apparent elimination half-life was 8 h and the mean cumulative elimination rate in urine within 48 h was 31–46%. Other inactive metabolites account for 7% of the dose. Half the administered dose is eliminated in feces within 72 h as ulifloxacin and 4% as prulifloxacin. Protein binding is 45%.
プルリフロキサシン 上流と下流の製品情報
原材料
準備製品
プルリフロキサシン 生産企業
Global( 318)Suppliers
123447-62-1(プルリフロキサシン)キーワード:
シクロペンテン
クレソキシムメチル
1-(1-アダマンチル)エチルアミン
4-ヒドロキシ-2,2,6,6-テトラメチルピペリジン
レボフロキサシン
2,2,6,6-テトラメチルピペリジン1-オキシル フリーラジカル
テトラブロモフルオレセイン
サリチル酸メチル
[1,2-フェニレンビス(イミノカルボノチオイル)]ビス(カルバミド酸)ジメチル
ガチフロキサシン
モキシフロキサシン
ノルフロキサシン
シプロフロキサシン
オフロキサシン
2-[[[[(4-メトキシ-6-メチル-1,3,5-トリアジン-2-イル)(メチル)アミノ]カルボニル]アミノ]スルホニル]安息香酸メチル
ポリメチルシルセスキオキサン
2-[[(4-メトキシ-6-メチル-1,3,5-トリアジン-2-イル)カルバモイル]スルファモイル]安息香酸メチル
ブロモメタン
- 123447-62-1
- 1h,4h-(1,3)thiazeto(3,2-a)quinoline-3-carboxylicacid,6-fluoro-1-methyl-7-(4-(
- 3-dioxol-4-yl)methyl)-1-piperazinyl)-4-oxo-(5-methyl-2-oxo-
- nm441
- Prulifloxacine
- PRULIFLOXACIN(FORRESEARCHONLY)
- (+/-)-7-{4-[(Z)-2,3-Dihydroxy-2-butenyl]-1-piperazinyl}-6-fluoro-1-methyl-4-oxo-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid cyclic carbonate
- 6-Fluoro-1-methyl-7-(4-(5-methyl-2-oxo-1,3-dioxelen-4-yl)methyl-1-piperazinyl)-4-oxo-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylic acid
- PRULIFLOXACIN
- SEA BUCKTHORN P.E 20%
- 6-Fluoro-1-Methyl-7-[4-[(5-Methyl-2-oxo-1,3-dioxol-4-yl)Methyl]-1-piperazinyl]-4-oxo-
- Quisnon
- Sword
- Prulifloxacin (Pruvel)
- Prulifloxacin,6-Fluoro-1-methyl-7-[4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl]-4-oxo-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid, NM441
- 6-fluoro-1-Methyl-7-(4-(5-Methyl-2-oxo-1,3-dioxelen-4-yl)Methyl-1-piperazinyl)-4-oxo-4h-(1,3)thiazeto(3
- 6-Fluoro-1-Methyl-7-(4-((5-Methyl-2-oxo-1,3-dioxol-4-yl)Methyl)piperazin-1-yl)-4-oxo-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid
- Prulioxacin-d8
- Prulifloxacin
(+/-)-7-{4-[(Z)-2,3-Dihydroxy-2-butenyl]-1-piperazinyl}-6-fluoro-1-methyl-4-oxo-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid cyclic carbonate
- 6-Fluoro-1-methyl-7-[4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl]-4-oxo-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid
- (1R)-6-fluoro-1-methyl-7-[4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl]-4-oxo-1H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid
- Prulifloxacin(NM441,AF3013)
- CS-1352
- Prulifloxacin, NM 441
- Pruvel
- PRULIFLOXACIN 99%
- Prulifloxacin>
- AF 3012
- 1H,4H-[1,3]Thiazeto[3,2-a]quinoline-3-carboxylic acid, 6-fluoro-1-methyl-7-[4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl]-4-oxo-
- hot selling Prulifloxacin
- Prulifloxacin USP/EP/BP
- プルリフロキサシン
- プルリフロキサシン (JAN)
- rac-(1R*)-6-フルオロ-1-メチル-7-[4-[(5-メチル-2-オキソ-1,3-ジオキソール-4-イル)メチル]ピペラジン-1-イル]-4-オキソ-4H-[1,3]チアゼト[3,2-a]キノリン-3-カルボン酸
- スオード