|(6R,7S)-7-(2-(((S)-2-氨基-2-羧乙基)硫基)乙酰胺基)-7-甲氧基-3-(((1-甲基-1H-四唑-5- (基)硫基)甲基)-8-氧代 5-硫杂-1-氮杂双环[4.2.0]辛烷-2-烯-2-羧酸钠盐|CsnPharm

CAS No.: 75498-96-3

Cefminox sodium/头孢米诺钠 Catalog No. CSN23269

Synonyms: MT-141;Cefminox Sodium;Meicelin

Cefminox Sodium (MT-141), the sodium salt form of cefminox, is a semi-synthetic cephalosporin with antibacterial activity.

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实验方案

技术信息

生物活性

描述Cefminox (Sodium) is a new cephamycin antibiotic possessing a D-amino acid moiety derived from D-cysteine at the C-7B side chain. Cefminox is active against a wide range of bacteria, especially Gram-negative and anaerobic bacteria. Cefminox shows excellent in vivo efficacy (ED50) which is higher than would be expected from its in vitro activity (MIC). Moreover, cefminox possesses more potent activity in suppression of bacterial regrowth than other cephems^[1]. Cefminox (Sodium) was the most active beta-lactam, with an MIC at which 50% of isolates are inhibited (MIC50) of 1.0 microg/ml and an MIC90 of 16.0 microg/ml. Cefminox was especially active against Bacteroides fragilis (MIC90, 2.0 microg/ml), Bacteroides thetaiotaomicron (MIC90, 4.0 microg/ml), fusobacteria (MIC90, 1.0 microg/ml), peptostreptococci (MIC90, 2.0 microg/ml), and clostridia, including Clostridium difficile (MIC90, 2.0 microg/ml) ^[2]. The use of a single preoperative dose of cefminox was similar in efficacy to 3 doses of cefoxitin administered every 4 hours, and that the serum and tissue concentrations attained provide adequate antibiotic coverage^[3]. Moreover, cefminox as a dual agonist of IP (Prostacyclin receptor) and PPARγ (peroxisome proliferator-activated receptor-gamma) that significantly inhibits PASMC proliferation by up-regulation of PTEN (phosphatase and tensin homolog) and cAMP ( cyclic adenosine monophosphate), suggesting that it has potential for treatment of PAH(pulmonary arterial hypertension) ^[4].
参考文献

[1] Watanabe S, Omoto S. Pharmacology of cefminox, a new bactericidal cephamycin. Drugs Exp Clin Res. 1990;16(9):461‐467
[2] Hoellman DB, Spangler SK, Jacobs MR, Appelbaum PC. In vitro activities of cefminox against anaerobic bacteria compared with those of nine other compounds. Antimicrob Agents Chemother. 1998;42(3):495‐501
[3] Garrido R, Novo A, Quintana S, et al. Cefminox versus Cefoxitin in Hysterectomy Prophylaxis : Clinical Efficacy and Serum and Tissue Concentrations. Clin Drug Investig. 1997;13(6):317‐325
[4] Xia J, Yang L, Dong L, et al. Cefminox, a Dual Agonist of Prostacyclin Receptor and Peroxisome Proliferator-Activated Receptor-Gamma Identified by Virtual Screening, Has Therapeutic Efficacy against Hypoxia-Induced Pulmonary Hypertension in Rats. Front Pharmacol. 2018;9:134. Published 2018 Feb 23

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8466 mL
- 9.2328 mL
- 18.4655 mL
- 5 mM
- 0.3693 mL
- 1.8466 mL
- 3.6931 mL
- 10 mM
- 0.1847 mL
- 0.9233 mL
- 1.8466 mL

技术信息

CAS号

75498-96-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H20N7NaO7S3

运输

蓝冰

分子量

541.55

别名

MT-141;Cefminox Sodium;Meicelin;头孢米诺钠

溶解度

DMSO	125.0 mg/mL (230.8 mM)
Water	123.0 mg/mL (227.1 mM)

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