Cloxacillin (sodium salt)
(Synonyms: 氯唑西林钠) 目录号 : GC43282
A β-lactam antibiotic
Cas No.:642-78-4
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cloxacillin is a semisynthetic β-lactamase inhibitor. It binds to and inactivates penicillin-binding proteins that cross-link peptidoglycans, which are structural components of bacterial cell walls. In vitro, addition of cloxacillin (0.50 μg/ml) almost completely inhibits B. megaterium growth. Cloxacillin inhibits recombinant type Ib penicillinase, P. vulgaris cephalosporinase, and C. freundii cephalosporinase (Kis = 15, 0.27, and 0.027 μM, respectively) as well as S. aureus and S. epidermidis growth (MICs = 0.2 and 0.2 μg/ml, respectively). In vitro, addition of cloxacillin (0.50 μg/ml) almost completely inhibits B. megaterium growth. Formulations containing cloxacillin have been used to treat infections caused by methicillin-sensitive staphylococci.
| Cas No. | 642-78-4 | SDF | |
| 别名 | 氯唑西林钠 | ||
| Canonical SMILES | CC1(C)[C@H](C([O-])=O)N2C([C@@H](NC(C3=C(C)ON=C3C4=CC=CC=C4Cl)=O)[C@@]2([H])S1)=O.[Na+] | ||
| 分子式 | C19H17ClN3O5S•Na | 分子量 | 457.9 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 16 mg/mL,Ethanol: 2 mg/mL,PBS (pH 7.2): 10 mg/mL | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1839 mL | 10.9194 mL | 21.8388 mL |
| 5 mM | 0.4368 mL | 2.1839 mL | 4.3678 mL |
| 10 mM | 0.2184 mL | 1.0919 mL | 2.1839 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。
Extravasation of Noncytotoxic Drugs: A Review of the Literature
Ann Pharmacother 2014 Jul;48(7):870-886.PMID:24714850DOI:10.1177/1060028014527820.
Objective: Extravasation is a potential complication associated with intravenous therapy administration. Inadvertent leakage of medications with vesicant properties can cause severe tissue necrosis, which can lead to devastating long-term consequences. Recognizing potential agents is an essential step in mitigating the risk of extravasation. Data source: A literature search was carried out using PubMed with the following key words: extravasation, soft tissue injury, phlebitis, and infiltration, from January 1961 through January 2014. Study selection and data extraction: The publications were screened manually and reviewed to identify reports for medications that included synonyms of the International Nonproprietary Name, while excluding antineoplastic agents, radiographic contrast material, investigational or nonmarketed drugs, and animal data, to yield 70 articles. Furthermore, reference citations from publications were also reviewed for relevance and yielded 4 articles. Data synthesis: We discovered 232 cases of extravasation involving 37 agents (in order of frequency): phenytoin, parenteral nutrition, calcium gluconate, potassium chloride, calcium chloride, dopamine, dextrose solutions, epinephrine, sodium bicarbonate, nafcillin, propofol, norepinephrine, mannitol, arginine, promethazine, vancomycin, tetracycline, dobutamine, vasopressin, sodium thiopental, acyclovir, amphotericin, ampicillin, Cloxacillin, gentamicin, metronidazole, oxacillin, penicillin, amiodarone, albumin, furosemide, lipids, lorazepam, immunoglobulin, morphine, and sodium valproate. Potential properties contributing to extravasation include the following: pH, osmolarity, diluent, vasoactive properties, and inactive ingredients. Antidotes and supportive care agents used in the management of these cases of extravasation include hyaluronidase, phentolamine, terbutaline, topical anesthetics (such as lidocaine and prilocaine cream), topical antimicrobials (such as silver sulfadiazine and chlorhexidine), topical debridement agents (collagenase ointment), topical steroids, and topical vasodilators (nitroglycerin). Conclusion: Data on the management of noncytotoxic extravasations is sparse, consisting primarily of case reports and anecdotal evidence. Fortunately, this adverse outcome is preventable and identification of vesicant agents plays a pivotal role. The intent of this review is to provide a reference identifying noncytotoxic vesicants and the management of extravasations associated with specific agents.
OXA-type beta-lactamases
Curr Pharm Des 1999 Nov;5(11):865-79.PMID:10539993doi
The OXA-type (oxacillin-hydrolysing) enzymes are widespread and have been mostly described in Enterobacteriaceae and in P. aeruginosa. They usually confer resistance to amino- and ureidopenicillin and possess high-level hydrolytic activity against Cloxacillin, oxacillin, and methicillin. Their activities are weakly inhibited by clavulanic acid but sodium chloride (NaCl) possesses a strong inhibition activity. Oxacillin-hydrolysing b-lactamases belong to Ambler class D and thus possess an active serine site as classes A and C b-lactamases. Overall amino-acid identities between class D and class A or class C b-lactamases is about 16%. Until now, 24 Ambler class D enzymes, named OXA-1 to OXA-22, AmpS and LCR-1, have been characterised, either by sequence and/or by biochemical analyses, but for none of them a three dimensional structure is yet available. While some oxacillinases present a significant degree of amino-acid identity (for example, OXA-1 and OXA-4; OXA-10 (PSE-2) derivatives; OXA-2 and OXA-3), most of them are only weakly related (20% to 30% amino-acid identity). Oxacillinases usually display a restricted-spectrum phenotype. However extension of their spectrum towards oxyimino cephalosporins and/or imipenem has recently been observed mostly as a consequence of point mutations in OXA-2 or OXA-10 derivatives. Their frequent plasmid- and/or integron-location provide them a mean for a wide diffusion.
Soft salt-mannitol agar-cloxacillin test: a highly specific bedside screening test for detection of colonization with methicillin-resistant Staphylococcus aureus
J Clin Microbiol 1998 Apr;36(4):986-9.PMID:9542922DOI:10.1128/JCM.36.4.986-989.1998.
The early detection of colonization with methicillin-resistant Staphylococcus aureus (MRSA) of patients in intensive-care units is an essential step in the strategy for preventing MRSA epidemics. In this study, tubes containing soft salt-mannitol agar with Cloxacillin (6 microg/ml) (SSMAC) were prepared for inoculation of clinical samples at patients' bedsides by personnel of an intensive-care unit. A total of 1,914 swabs from different sample sites of 81 patients were dipped into SSMAC tubes, and after 24 h of incubation (in an incubator located near the intensive-care unit), an evident color change was considered by the intensive-care-unit personnel to be an MRSA alarm. Sixty-three (3.3%) SSMAC tubes were considered positive for MRSA, 1,827 (95.4%) were considered negative, and 24 (1.2%) were considered intermediate. Compared with values for parallel conventional surveillance cultures for MRSA, excluding tubes with intermediate results, the SSMAC test had a sensitivity of 72.7%, a specificity of 99.2%, a positive predictive value of 76.2%, and a negative predictive value of 99.0%. When intermediate tubes were considered positive, the corresponding values were 75.3, 98.2, 63.2, and 99.0%, respectively. The sensitivity and specificity values of the test to identify MRSA-colonized patients were 89.4 and 100%, respectively. Oropharyngeal and naris specimens were the most reliable samples for MRSA detection. False-negative results were frequent in bronchial aspirates with low (< 10(3) to 10(6) CFU/ml) MRSA counts. False-positive results were mainly due to methicillin-resistant Staphylococcus haemolyticus. The SSMAC tube is a useful, rapid, and inexpensive tool for the early identification of MRSA-colonized patients and, consequently, for the implementation of measures to prevent the spread of MRSA.
Beta-lactamase activity in Shigella sonnei
Antimicrob Agents Chemother 1976 May;9(5):776-9.PMID:782355DOI:10.1128/AAC.9.5.776.
The basis of ampicillin resistance in Shigella sonnei was analyzed for a number of isolates. Most isolates that were resistant to ampicillin and cephalothin failed to transfer resistance. Isolates resistant to cephalothin and ampicillin were inhibited by mecillinam, cefamandole, and cefoxitin. Six strains were selected for study. These differed on the basis of inhibition by 10 beta-lactam antibiotics and on differences in beta-lactamase activity. There was no correlation between the inhibitory concentration of antibiotic and the amount of antibiotic hydrolyzed. Use of sodium chloride and Cloxacillin inhibition and acrylamide electrophoresis demonstrated that ampicillin resistance in Shigella is mediated by a number of different beta-lactamases. Organisms can contain more than one type of beta-lactamase.
LC-MS study of the heat degradation of veterinary antibiotics in raw milk after boiling
Food Chem 2018 Nov 30;267:178-186.PMID:29934154DOI:10.1016/j.foodchem.2017.11.041.
The aim of our study was to examine the degradation of veterinary antibiotics in milk during boiling. Raw cow milk samples were fortified with the target compounds and boiled for various short time-intervals prevailing in household practice. Antibiotic concentrations were determined by LC-MS/MS measurements. Degradation rate constants, half-lives and degradation percentages were calculated. Cefoperazone and Cloxacillin proved to be the less and the most heat-stable substance, with 78.3% and 9.6% degradation in 300 s respectively. Aminoglicosides exhibited intermediate (33.8-43.6%), tetracycline (30.4%) and trimethoprim (22.6%) intermediate to high heat stability. The results demonstrate that antibiotic residues possibly present in raw milk exhibit high heat stability when treated for few seconds at around 100 °C. Keeping the milk at this temperature for at least two minutes would allow varying decrease in the amount of some compounds, but does not totally eliminate the potential risks to the consumer's health.