Pefloxacin鏄姉鑿屽寲鍚堢墿锛岄€氳繃鎶戝埗DNA鏃嬭浆閰舵潵闃绘柇DNA澶嶅埗銆侟/div>
| 鐢熺墿娲绘€?/td> |
Pefloxacin mesylate is a an antibacterial agent and preventsbacterialDNA replication by inhibiting DNA gyrase (topoisomerse) Target: DNA gyrase Pefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threateningbacterialinfections. Pefloxacin is commonly referred to as afluoroquinolone (or quinolone) drug and is a member of the fluoroquinolone class of antibacterials. It is an analog of norfloxacin. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones. Pefloxacin is extensively prescribed in France. Pefloxacin has not been approved for use in the United States. The bactericidal action of pefloxacin results from interference with the activity of thebacterialenzymes DNA gyrase andtopoisomeraseIV, which are needed for the transcription and replication ofbacterialDNA. DNA gyrase appears to be the primaryquinolonetarget for gram-negative bacteria.TopoisomeraseIV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of thebacterialchromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
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| IC50& Target |
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| 鍒嗗瓙閲廃/td> |
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| 鎬х姸 |
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| Formula |
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| CAS 鍙饵/td> |
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| 涓枃鍚嶇О |
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| 杩愯緭鏉′欢 |
Room temperature in continental US; may vary elsewhere.
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| 鍌ㄥ瓨鏂瑰紡 |
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| 婧惰В鎬ф暟鎹?/td> |
In Vitro:
H2O : 鈮 100 mg/mL(232.85 mM)
DMSO : 12.5 mg/mL(29.11 mM;Need ultrasonic)
*"鈮? means soluble, but saturation unknown.
閰嶅埗鍌ㄥ娑秉/div>
| 娴撳害婧跺墏浣撶Н璐ㄩ噺 |
1 mg |
5 mg |
10 mg |
| 1 mM |
2.3285 mL |
11.6425 mL |
23.2851 mL |
| 5 mM |
0.4657 mL |
2.3285 mL |
4.6570 mL |
| 10 mM |
0.2329 mL |
1.1643 mL |
2.3285 mL |
*
璇锋牴鎹骇鍝佸湪涓嶅悓婧跺墏涓殑婧惰В搴﹂€夋嫨鍚堥€傜殑婧跺墏閰嶅埗鍌ㄥ娑诧紱涓€鏃﹂厤鎴愭憾娑诧紝璇峰垎瑁呬繚瀛橈紝閬垮厤鍙嶅鍐昏瀺閫犳垚鐨勪骇鍝佸け鏁圏/b>銆侟/span>
鍌ㄥ娑茬殑淇濆瓨鏂瑰紡鍜屾湡闄愶細-80鈩? 6 months; -20鈩? 1 month (sealed storage, away from moisture)銆侟/span>-80鈩 鍌ㄥ瓨鏃讹紝璇峰湪 6 涓湀鍐呬娇鐢紝-20鈩 鍌ㄥ瓨鏃讹紝璇峰湪 1 涓湀鍐呬娇鐢ㄣ€侟/span>
In Vivo:
璇锋牴鎹偍鐨勫疄楠屽姩鐗╁拰缁欒嵂鏂瑰紡閫夋嫨閫傚綋鐨勬憾瑙ｆ柟妗堛€備互涓嬫憾瑙ｆ柟妗堥兘璇峰厛鎸夌収In Vitro鏂瑰紡閰嶅埗婢勬竻鐨勫偍澶囨恫锛屽啀渚濇娣诲姞鍔╂憾鍓傦細
鈥斺€斾负淇濊瘉瀹為獙缁撴灉鐨勫彲闈犳€э紝婢勬竻鐨勫偍澶囨恫鍙互鏍规嵁鍌ㄥ瓨鏉′欢锛岄€傚綋淇濆瓨锛涗綋鍐呭疄楠岀殑宸ヤ綔娑诧紝寤鸿鎮ㄧ幇鐢ㄧ幇閰嶏紝褰撳ぉ浣跨敤锛 浠ヤ笅婧跺墏鍓嶆樉绀虹殑鐧近br/>鍒嗘瘮鏄寚璇ユ憾鍓傚湪鎮ㄩ厤鍒剁粓婧舵恫涓殑浣撶Н鍗犳瘮锛涘鍦ㄩ厤鍒惰繃绋嬩腑鍑虹幇娌夋穩銆佹瀽鍑虹幇璞★紝鍙互閫氳繃鍔犵儹鍜?鎴栬秴澹扮殑鏂瑰紡鍔╂憾
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1.
璇蜂緷搴忔坊鍔犳瘡绉嶆憾鍓傦細 PBS
Solubility: 150 mg/mL (349.28 mM); Clear solution; Need ultrasonic
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2.
璇蜂緷搴忔坊鍔犳瘡绉嶆憾鍓傦細 10% DMSO40%PEG3005%Tween-8045% saline
Solubility: 鈮 1.25 mg/mL (2.91 mM); Clear solution
姝ゆ柟妗堝彲鑾峰緱 鈮 1.25 mg/mL (2.91 mM锛岄ケ鍜屽害鏈煡) 鐨勬緞娓呮憾娑层€侟/p>
浠 1 mL 宸ヤ綔娑蹭负渚嬶紝鍙 100 渭L 12.5 mg/mL 鐨勬緞娓 DMSO 鍌ㄥ娑插姞鍒 400 渭L PEG300 涓紝娣峰悎鍧囧寑锛涘悜涓婅堪浣撶郴涓姞鍏?0 渭L Tween-80锛屾贩鍚堝潎鍖€锛涚劧鍚庣户缁姞鍏 450 渭L鐢熺悊鐩愭按瀹氬鑷 1 mL銆侟/p>
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3.
璇蜂緷搴忔坊鍔犳瘡绉嶆憾鍓傦細 10% DMSO90% (20%SBE-尾-CDin saline)
Solubility: 鈮 1.25 mg/mL (2.91 mM); Clear solution
姝ゆ柟妗堝彲鑾峰緱 鈮 1.25 mg/mL (2.91 mM锛岄ケ鍜屽害鏈煡) 鐨勬緞娓呮憾娑层€侟/p>
浠 1 mL 宸ヤ綔娑蹭负渚嬶紝鍙 100 渭L 12.5 mg/mL 鐨勬緞娓 DMSO 鍌ㄥ娑插姞鍒 900 渭L20% 鐨 SBE-尾-CD 鐢熺悊鐩愭按姘存憾娑秉/span>涓紝娣峰悎鍧囧寑銆侟/p>
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4.
璇蜂緷搴忔坊鍔犳瘡绉嶆憾鍓傦細 10% DMSO90%corn oil
Solubility: 鈮 1.25 mg/mL (2.91 mM); Clear solution
姝ゆ柟妗堝彲鑾峰緱 鈮 1.25 mg/mL (2.91 mM锛岄ケ鍜屽害鏈煡) 鐨勬緞娓呮憾娑诧紝姝ゆ柟妗堜笉閫傜敤浜庡疄楠屽懆鏈熷湪鍗婁釜鏈堜互涓婄殑瀹為獙銆侟/p>
浠 1 mL 宸ヤ綔娑蹭负渚嬶紝鍙 100 渭L 12.5 mg/mL 鐨勬緞娓 DMSO 鍌ㄥ娑插姞鍒 900 渭L鐜夌背娌逛腑锛屾贩鍚堝潎鍖€銆侟/p>
*浠ヤ笂鎵€鏈夊姪婧跺墏閮藉彲鍦ㄦ湰缃戠珯閫夎喘銆侟/span>
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