| Description | Cefoselis Sulfate (FK 037 Sulfate) is a widely used beta-lactam antibiotic. |
| In vitro | Cefoselis以浓度依赖的方式抑制GABA诱导的电流,IC50为185 mM。[1] Cefoselis对MSSA分离物表现出比其他化合物更优越的抗葡萄球菌活性,但与Cefepime和Cefpirome在对多重耐药肠杆菌科细菌的活性上相当。[2] Cefoselis在大脑细胞外液中的出现与其血液中的浓度成比例,呈剂量依赖性。[3] Cefoselis是一种新的静脉注射用头孢菌素,对临床分离的革兰氏阳性和阴性需氧细菌均有效。[4] |
| In vivo | Cefoselis 在正常大鼠体内引起外源性谷氨酸浓度的大幅升高。[3] Cefoselis (50 mg/动物) 引起的惊厥可通过预先治疗5-甲基-10,11-二氢-5H-二苯并[a,d]环庚烯-5,10-亚胺(MK-801)、地西泮和苯巴比妥(ED(50) 值(mg/kg)分别为0.78、1.59 和33.0)来预防,但卡马西平或苯妥英则无此效果。[5] |
| Synonyms | FK 037 Sulfate, FK-037, 硫酸头孢噻利 |
| molecular weight | 620.64 |
| Molecular formula | C19H22N8O6S2·H2SO4 |
| CAS | 122841-12-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 27.5 mg/mL (44.31 mM) |
| References | 1. Sugimoto M, et al. Br J Pharmacol, 2002, 135(2), 427-432. 2. Giamarellos-Bourboulis EJ, et al. Diagn Microbiol Infect Dis, 2000, 36(3), 185-191. 3. Ohtaki K, et al. J Neural Transm, 2004, 111(12), 1523-1535. 4. Yamada K, et al. J Infect Chemother, 2012, 18(4), 472-478. 5. Yamazaki S, et al. Pharmacol Biochem Behav, 2002, 74(1), 53-59. |