Cloxacillin (sodium salt)是一种口服有效的抗菌剂和β-内酰胺酶抑制剂，IC50值为0.04µM。
Cas No.:642-78-4
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Cloxacillin (sodium salt) is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 value of 0.04µM [1]. Cloxacillin inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins and is resistant to the beta-lactamase enzyme produced by S. aureus [2]. Cloxacillin is widely used as an antibiotic in veterinary medicine against S. aureus and can be combined with plant essential oils to kill drug-resistant bacteria[3].
In vitro, Cloxacillin treatment for 5min significantly inhibited organic anion transporter (OAT) 1, OAT3, and OAT4 activities in OAT-overexpressing HEK293 cells with IC50 values of 550µM, 13µM, and 21µM, respectively[4]. Cloxacillin treatment (0.015625μg/ml) combined with thioridazine (0.25μg/ml) and tetracycline (0.03125μg/ml) for 6h significantly inhibited the expression of MAPK/NF-κB/NLRP3 proteins in RAW264.7 cells induced with S. aureus[5].
In vivo, Cloxacillin treatment via intraperitoneal injection (7.5mg/mouse; twice daily) for 3 day combined with IL-15 neutralizing antibodies, reduced synovitis and bone erosions in S. aureus-induced arthritis of mice[6].
References:
[1] Lupiola-Gómez P A, Gonzalez-Lama Z, Tejedor-Junco M T, et al. Group 1 β-lactamases of Aeromonas caviae and their resistance to β-lactam antibiotics[J]. Canadian journal of microbiology, 2003, 49(3): 207-215.
[2] Mani S S R, Iyyadurai R. Cloxacillin induced agranulocytosis: a rare adverse event of a commonly used antibiotic[J]. International Journal of Immunopathology and Pharmacology, 2017, 30(3): 297-301.
[3] Buldain D, Buchamer A V, Marchetti M L, et al. Combination of cloxacillin and essential oil of Melaleuca armillaris as an alternative against Staphylococcus aureus[J]. Frontiers in Veterinary Science, 2018, 5: 177.
[4] Lalanne S, Le Vée M, Lemaitre F, et al. Differential interactions of the β‐lactam cloxacillin with human renal organic anion transporters (OATs)[J]. Fundamental & Clinical Pharmacology, 2020, 34(4): 476-483.
[5] Zhou H, Luan W, Wang Y, et al. The combination of cloxacillin, thioridazine and tetracycline protects mice against Staphylococcus aureus peritonitis by inhibiting α-Hemolysin-induced MAPK/NF-κB/NLRP3 activation[J]. International Journal of Biological Macromolecules, 2022, 198: 1-10.
[6] Bergmann B, Jirholt P, Henning P, et al. Antibiotics with Interleukin-15 inhibition reduce joint inflammation and bone erosions but not cartilage destruction in Staphylococcus aureus-induced arthritis[J]. Infection and Immunity, 2018, 86(5): 10.1128/iai. 00960-17.
Cloxacillin (sodium salt)是一种口服有效的抗菌剂和β-内酰胺酶抑制剂，IC50值为0.04µM[1]。Cloxacillin通过与青霉素结合蛋白结合抑制细菌细胞壁合成，并对金黄色葡萄球菌产生的β-内酰胺酶具有抗性[2]。Cloxacillin在兽医学中被广泛用作抗金黄色葡萄球菌的抗生素，并可与植物精油联合使用以杀灭耐药细菌[3]。
在体外，Cloxacillin处理5分钟显著抑制了过表达有机阴离子转运体（OAT）1、OAT3和OAT4的HEK293细胞中的相应活性，IC50值分别为550µM、13µM和21µM[4]。Cloxacillin（0.015625µg/ml）联合thioridazine（0.25µg/ml）和四环素（0.03125µg/ml）处理6小时，显著抑制了金黄色葡萄球菌诱导的RAW264.7细胞中MAPK/NF-κB/NLRP3蛋白的表达[5]。
在体内，每日两次腹腔注射Cloxacillin（7.5mg/只小鼠）连续3天，联合IL-15中和抗体治疗，减轻了金黄色葡萄球菌诱导的小鼠关节炎的滑膜炎和骨侵蚀[6]。
| Cell experiment [1]: | |
Cell lines | RAW264.7 cells |
Preparation Method | RAW264.7 cells were cultured in high-glucose DMEM medium supplemented with 10% fetal bovine serum (FBS) at 37℃ in the presence of 5% CO2. RAW264.7 cells (1×106) were exposed to S. aureus 8325–4/DU1090 (E:T ratio, 5:1) or pure Hlα (100μg/ml). The drug combination (Cloxacillin: 0.015625μg/ml; thioridazine: 0.25μg/ml; tetracycline: 0.03125μg/ml) was added to the cells and incubated at 37°C for 6h. Total protein was collected, and the protein was subjected to SDS-PAGE. |
Reaction Conditions | 0.015625μg/ml; 6h |
Applications | Cloxacillin treatment combined with thioridazine and tetracycline significantly inhibited the expression of MAPK/NF-κB/NLRP3 proteins in RAW264.7 cells induced with S. aureus. |
| Animal experiment [2]: | |
Animal models | Female C57BL/6 mice |
Preparation Method | Female C57BL/6 mice (8-week-old) were maintained under standard conditions of temperature and light and were fed laboratory chow and water ad libitum. Female wild-type C57BL/6 mice were inoculated i.v. in the tail vein with 0.8×108 CFU S. aureus LS-1/mouse in a total volume of 200μl of phosphate-buffered saline (PBS). To determine the number of bacteria injected, viable counts were performed. The IL-15 neutralizing antibodies (25μg/mouse) were injected intraperitoneally at days 3, 6, and 10 after bacterial inoculation. Intraperitoneal injections of Cloxacillin (7.5mg/mouse) were given twice daily from day 3 and stopped at day 6, when flucloxacillin was added to the drinking water (70mg/kg). Mouse knee tissues were collected for analysis. |
Dosage form | 7.5mg/mouse; twice daily for 3 days; i.p. |
Applications | Cloxacillin treatment combined with antibodies reduced synovitis and bone erosions in S. aureus-induced arthritis of mice. |
References: | |
| 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 | 436.8 μL | 2.1839 mL | 4.3678 mL |
| 10 mM | 218.4 μL | 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet