Cefradine (Cephradine)
(Synonyms: 头孢拉定; Cefradine; SQ-11436) 目录号 : GC32181
A β-lactam cephalosporin antibiotic
Cas No.:38821-53-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cefradine is an orally bioavailable β-lactam cephalosporin antibiotic.1 It is active against S. pyogenes, E. coli, K. pneumoniae, and E. cloacae (MICs = 0.04, 9.4, 9.4, and 6.3 μg/ml, respectively). Cefradine is also active against clinical isolates of S. aureus (MICs = 0.8-6 μg/ml) and S. pyogenes (MICs = 0.1-0.4 μg/ml), as well as H. influenzae, E. coli, and K. pneumoniae (MICs = 6.2-12.5 μg/ml).2 It increases survival in mouse models of systemic lethal infection by S. pyogenes, E. coli, K. pneumoniae, or E. cloacae (ED50s = 5, 37, 122, and 50 mg/kg, respectively), as well as by penicillin-susceptible or -resistant strains of S. aureus (ED50s = 18 and 91 mg/kg, respectively).1 Formulations containing cefradine have previously been used in the treatment of respiratory and urinary tract infections, skin infections, and otitis media.
1.Miraglia, G.J., Renz, K.J., and Gadebusch, H.H.Comparison of the chemotherapeutic and pharmacodynamic activities of cephradine, cephalothin, and cephaloridine in miceAntimicrob. Agents Chemother.3(2)270-273(1973) 2.Shibl, A.M., and Durgham, S.M.In-vitro evaluation of a new oral cephalosporin, cefroxadine (CGP 9000)J. Chemother.2(1)8-10(1990)
| Cas No. | 38821-53-3 | SDF | |
| 别名 | 头孢拉定; Cefradine; SQ-11436 | ||
| Canonical SMILES | O=C(C(N12)=C(C)CS[C@]2([H])[C@H](NC([C@H](N)C3=CCC=CC3)=O)C1=O)O | ||
| 分子式 | C16H19N3O4S | 分子量 | 349.4 |
| 溶解度 | DMSO : ≥ 3.6 mg/mL (10.30 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.862 mL | 14.3102 mL | 28.6205 mL |
| 5 mM | 0.5724 mL | 2.862 mL | 5.7241 mL |
| 10 mM | 0.2862 mL | 1.431 mL | 2.862 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
[Non-Necrotizing Acute Dermo-Hypodermal Infections: Erysipela and Infectious Cellulitis]
Acta Med Port 2021 Mar 1;34(3):217-228.PMID:33971117DOI:10.20344/amp.12642.
Non-necrotizing acute dermo-hypodermal infections are infectious processes that include erysipela and infectious cellulitis, and are mainly caused by group A 尾-haemolytic streptococcus. The lower limbs are affected in more than 80% of cases and the risk factors are disruption of cutaneous barrier, lymphoedema and obesity. Diagnosis is clinical and in a typical setting we observe an acute inflammatory plaque with fever, lymphangitis, adenopathy and leucocytosis. Bacteriology is usually not helpful because of low sensitivity or delayed positivity. In case of atypical presentations, erysipela must be distinguished from necrotizing fasciitis and acute vein thrombosis. Flucloxacillin and Cefradine remain the first line of treatment. Recurrence is the main complication, so correct treatment of the risk factors is crucial.
Cefradine blocks solar-ultraviolet induced skin inflammation through direct inhibition of T-LAK cell-originated protein kinase
Oncotarget 2016 Apr 26;7(17):24633-45.PMID:27016423DOI:10.18632/oncotarget.8260.
Skin inflammation, and skin cancer induced by excessive solar ultraviolet (SUV) is a great threat to human health. SUV induced skin inflammation through activating p38 mitogen-activated protein kinase (p38) and c-Jun N-termeinal kinases (JNKs). T-LAK cell-originated protein kinase (TOPK) plays an important role in this process. Herein, the clinical data showed TOPK, phospho-p38, phospho-JNKs were highly expressed in human solar dermatitis. Ex vivo studies showed that SUV induced the phosphorylation of p38 and JNKs in HaCat and JB6 cells in a dose and time dependent manner. Molecule docking model indicated Cefradine, an FDA-approved cephalosporin antibiotic, directly binds with TOPK. The result of in vitro binding assay verified Cefradine can directly bind with TOPK. In vitro kinase results showed Cefradine can inhibit TOPK activity. Ex vivo studies further showed Cefradine inhibited SUV-induced the phosphorylation level of p38, JNKs and H2AX through inhibiting TOPK activity in a dose and time dependent manner, and Cefradine inhibited the secretion of IL6 and TNF-伪 in HaCat and JB6 cells. In vivo studies showed that Cefradine down-regulated SUV-induced the phosphorylation of p38, JNKs and H2AX and inhibited the secretion of IL6 and TNF-伪 in Babl/c mice. These results indicated that Cefradine can inhibit SUV-induced skin inflammation by blocking TOPK signaling pathway, and TOPK is an effective target for suppressing inflammation induced by SUV irradiation.
Effects of chronic exposure to cefadroxil and Cefradine on Daphnia magna and Oryzias latipes
Chemosphere 2017 Oct;185:844-851.PMID:28735237DOI:10.1016/j.chemosphere.2017.07.085.
Cefadroxil and Cefradine have frequently been detected in surface waters, however toxicological studies in aquatic organisms have mostly been limited to acute lethal effects. In the present study, endocrine disruption caused by cefadroxil and Cefradine, and its underlying mechanism were investigated by chronic exposure of Daphnia magna (21 d) and Oryzias latipes (120 d). In medaka fish, the effects on growth, mortality, and reproduction, as well as on the levels of hormones and genes related to the hypothalamic-pituitary-gonad (HPG) axis, were investigated after 120 d exposure. In D. magna, the chronic effects on growth were observed at the highest concentration of 83.0 mg L-1 cefadroxil and 80.8 mg L-1 Cefradine. The growth of juvenile fish was significantly impaired by exposure to Cefradine. Following exposure to cefadroxil and Cefradine for 120 d, sex-dependent changes in E2 hormones were observed and their levels were supported by the regulation of genes along the HPG axis. We found that chronic exposure to cefadroxil and Cefradine impaired growth and reproduction in a freshwater invertebrate and fish, and altered the levels of sex hormones and genes associated with the HPG axis in fish.
Study on the interaction mechanism between Cefradine and Chlamydomonas reinhardtii in water solutions under dark condition
Ecotoxicol Environ Saf 2018 Sep 15;159:56-62.PMID:29730409DOI:10.1016/j.ecoenv.2018.04.068.
Our research investigated the hormesis effect of Cefradine on the specific growth rates (渭) of single-celled algae (Chlamydomonas reinhardtii) from aqueous solutions. We found the specific growth rate of C. reinhardtii slightly increased with Cefradine concentrations within the range 0.5-10 mg/L. Effects of algae density, initial solution pH, and temperature on the adsorption batch assays were investigated. The optimum conditions for Cefradine adsorption occurred at a density of 5 脳 106 algae cells/mL, a solution pH of 7.0, and a temperature of 25.0 掳C. A Box-Behnken design was employed to evaluate correlations between influential factors and Cefradine adsorption. The results showed a significant interaction between algae density and temperature. The maximum removal rate could reach 50.13% under the optimal conditions. Additionally, the adsorption mechanisms were explored through Langmuir and Freundlich isotherm equations, adsorption kinetics, and thermodynamics. The results suggested that the adsorption process was monolayer, spontaneous, and endothermic with an increase in randomness at the algae-solution interface, which followed a pseudo-second-order model. All the data indicated that the alga performed a better removal capacity in the antibiotic-containing wastewater treatment process. This study lays the groundwork for a better understanding of the interaction mechanism between Cefradine and Chlamydomonas reinhardtii in water solutions under dark condition.
An Open-Label, Randomized, 2-Way, Crossover Bioequivalence Study of Cefradine Capsules in Healthy Chinese Volunteers
Clin Pharmacol Drug Dev 2021 Dec;10(12):1478-1484.PMID:34148297DOI:10.1002/cpdd.991.
The purpose of this study was to evaluate whether test Cefradine capsules and reference Cefradine capsules were bioequivalent in healthy Chinese volunteers. An open-label, randomized, biperiodic, crossover design was used. In each of the 2 study periods (separated by a 1-week washout period), 250-mg single doses of either the test or reference Cefradine capsule were administered to study participants under fasted and fed conditions. Blood samples were collected at intervals from predose to 8 hours afterward. In the fasting study, the 90% confidence intervals (90%CI) of the Cmax , AUC0-8h , and AUC0-鈭?for the test and reference preparations were 93.7%-112.2%, 94.6%-100.8%, and 94.7%-100.9%, respectively. In the fed study, the 90%CI of the Cmax , AUC0-8h , and AUC0-鈭?for the test and reference preparations was 81.0%-99.1%, 100.5%-106.3%, and 100.5%-105.9%, respectively. The results showed that the test Cefradine capsules and the reference formulation are bioequivalent under both fasting and fed conditions.