厄他培南钠
| 中文名称 | 厄他培南钠 |
|---|---|
| 中文同义词 | 尔他培南钠;(4R,5S,6S)-3-[[(3S,5S)-5-[[(3-羧基苯基)氨基甲酰基]吡咯烷-3-基]硫-6-(1-羟基乙基)-4-甲基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-甲酸钠盐;厄他培南钠盐;厄他培南粗品;厄他培南钠;(4R,5R,6S)-3-[(3S,5S)-5-[(3-羧基苯基)氨基甲酰基]吡咯烷-3-基]硫-6-(1-羟乙基)-4-甲基-7-氧代-1-氮杂双环[3.2.0]庚-2-烯-2-甲酸钠盐/厄他培南钠盐/尔他培南钠盐/呃他培南钠盐;98%规格厄他培南钠;(4R,5S,6S)-3-(((3S,5S)-5-((3-羧基苯基)氨基甲酰基)吡咯烷-3-基)硫基)-6-((R)-1-羟乙基)-4-甲基-7-氧代-1-氮杂双环[3.2.0]庚烷-2-烯-2-甲酸单钠盐 |
| 英文名称 | Ertapenem sodium |
| 英文同义词 | 1-Azabicyclo(3.2.0)hept-2-ene-2-carboxylic acid, 3-(((3S,5S)-5-(((3-ca rboxyphenyl)amino)carbonyl)-3-pyrrolidinyl)thio)-6-((1R)-1-hydroxyethy l)-4-methyl-7-oxo-, monosodium salt, (4R,5S,6S)-;(4R,5S,6S)-3-[[(3S,5S)-5-[[(3-Carboxyphenyl)amino]carbonyl]-3-pyrrolidinyl]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid sodium salt (1:1);L 749345;EtapeneM,Invanz,MK-0826,L-749,345;EtapeneM;ErtapeneM Crude;Etapenem sodium;Ertapenem sodium, >=97% |
| CAS号 | 153773-82-1 |
| 分子式 | C22H26N3NaO7S |
| 分子量 | 499.51 |
| EINECS号 | 1308068-626-2 |
| 相关类别 | 抗生素及抗病毒;原料药;医药原料;抗生素;中间体;医用原料;医药原料药;原料;化工原料;医药、农药及染料中间体;化学试剂;通用生化试剂-抗生素;有机化学;精细化工原料 |
| Mol文件 | 153773-82-1.mol |
| 结构式 |  |
厄他培南钠 性质
| 熔点 | >174oC (dec.) |
|---|---|
| 储存条件 | -70°C |
| 溶解度 | 可溶于DMSO（轻微）、甲醇（轻微）、水（轻微、超声处理） |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| 水溶解性 | Fully miscible in water. Soluble in DMSO. |
| 稳定性 | 吸湿性、温度敏感 |
Ertapenem sodium (L-749345; MK-826) 属于长效的碳青霉烯，是一种 β-内酰胺抗生素，具有广泛的抗菌谱。Ertapenem sodium 对革兰氏阳性菌和革兰氏阴性菌均有活性，包括肠杆菌科、肺炎链球菌和大多数种类的厌氧菌。
Ertapenem sodium inhibits
Streptococcus pneumoniae
with MIC
50
s values < 1mg/L.
Ertapenem sodium exhibits a bactericidal mode of action as shown by time-killing curves and exhibits a short postantibiotic effect (PAE) of 1.4-2.6 h against the Gram-positive strains but no PAE against Gram-negative strains.
Ertapenem sodium (50 mg/kg; s.c.; q6h; for 24 hours) shows substantial bactericidal activity against
S. pneumoniae
in the murine thigh infection model.
Ertapenem sodium exhibits an AUC
0-24
of 586 mg•h/L, C
max
of 140 mg/L following subcutaneous injection (mice 50 mg/kg).
| Animal Model: | Specific-pathogen-free female ICR mice (~25 g), thigh infection model |
| Dosage: | 50 mg/kg |
| Administration: | Subcutaneous injection, q6h, for 24 hours |
| Result: | Showed substantial bactericidal activities. |
| Animal Model: | Specific-pathogen-free female ICR mice (~25 g), thigh infection model |
| Dosage: | 20 mg/kg, 50 mg/kg, 100 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Subcutaneous injection |
| Result: | AUC 0-24 (586 mg•h/L), C max (140 mg/L) at 50 mg/kg q6h dosing regimen. |