水合加替沙星
Gatifloxacin sesquihydrate
| 货号 | 包装规格 | 纯度/级别 | 交货周期 | 价格 | 数量 |
|---|---|---|---|---|---|
| YB61886-1g | 1g | 95% | 现货 | ||
| YB61886-5g | 5g | 95% | 现货 | ||
| YB61886-25g | 25g | 95% | 现货 | ||
| YB61886-100g | 100g | 95% | 现货 |
| 中文名称 | 水合加替沙星 |
|---|---|
| 英文名称 | Gatifloxacin sesquihydrate |
| 别名 | Gatifloxacin sesquihydrate, (±)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazin |
| Cas No. | 180200-66-2 |
| MDL No. | MFCD22373645 |
| 精确分子量 | 804.35057 |
| Smiles | CC1NCCN(C2C(OC)=C3N(C4CC4)C=C(C(O)=O)C(=O)C3=CC=2F)C1.CC1NCCN(C2C(OC)=C3N(C4CC4)C=C(C(O)=O)C(=O)C3=CC=2F)C1.O.O.O |
| 密度 | 1.386 g/cm3 |
|---|---|
| 信号词 | Warning |
| 危险类别(旧) | 20/21/22 |
| 熔点 | 607.8ºC at 760 mmHg |
| 沸点 | 684℃ |
| 海关编码 | 2933990090 |
| 特性 | * |
| 安全说明(旧) | 36/37 |
| 水溶解性 | DMSO: 2 mg/mL, clear (Warmed) |
| 符号 | GHS07 |
| 存储要求 | 2-8°C |
| 闪点 | 321.4ºC |
水合加替沙星是一种口服氟喹诺酮类广谱抗生素，通过抑制细菌的DNA旋转酶和拓扑异构酶IV发挥作用，并增强了对革兰氏阳性菌及厌氧菌的抗菌活性。
用途
水合加替沙星可用于治疗眼部感染，且未见引起光毒性反应。
生物活性
水合加替沙星(AM-1155 sesquihydrate) 是一种有效的氟喹诺酮类抗生素 (antibiotic)，具有广谱抗菌活性。其可抑制细菌 II 型拓扑异构酶 (type II topoisomerases) (IC50=13.8 μg/ml; 金黄色葡萄球菌拓扑异构酶 IV) 和大肠杆菌 DNA 解旋酶 (IC50=0.109 μg/ml)。其在动物模型中，可用于细菌性结膜炎的研究。
靶点
|
Topoisomerase II 36.7 μM (IC 50 ) |
体外研究
Gatifloxacin sesquihydrate is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with IC 50 values of 13.8 μg/ml, 0.109 μg/ml, and 265 μg/ml, respectively.Gatifloxacin sesquihydrate is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with MIC values of 0.05 μg/ml, 0.0063 μg/ml, and 122 μg/ml, respectively.Gatifloxacin sesquihydrate exhibits antibacterial activities for wild-type strains (MS5935, MS5952, MR5867 and MR6009) the first-, second-, third-, and fourth-step mutants with MIC values of 0.05 to 0.10 μg/ml, 0.20 μg/ml, 1.56 to 3.13 μg/ml, 1.56 to 6.25 μg/ml, and 50 to 200 μg/ml, respectively. Gatifloxacin sesquihydrate displays the most potent activity against the second- and third-step mutants (MS5952, MR5867 and MR6009) except for the second-step mutant of strain MS5935.Gatifloxacin sesquihydrate has potent activity against norA transformant NY12 (MIC, 0.39 μg/ml).Gatifloxacin sesquihydrate (20-100 μM; 72 hours) significantly decreases insulin content to 60% at Day 1, and continues to be reduced to 50.1% and 44.7% at Day 3 by 20 μM and 100 μM Gatifloxacin sesquihydrate, respectively.
体内研究
Gatifloxacin sesquihydrate (subcutaneous injection; 100 mg/kg; 3 times a day; 30 days) significantly decreases the number of lesions in mouse footpad with Nocardia brasiliensis .
| Animal Model: | Female BALB/c mice with Nocardia brasiliensis in the right hind footpad |
| Dosage: | 100 mg/kg |
| Administration: | Subcutaneous injection; 3 times a day; 30 days |
| Result: | Reduced the production of lesions in mice. |
