Cloxacillin 是一种口服有效的抗菌剂和β-lactamase抑制剂，其IC50值为 0.04 μM。Cloxacillin 可通过抑制MAPKs、NF-кB和NLRP3相关蛋白的激活从而抑制金黄色葡萄球菌所引起的炎症反应。
| 生物活性 | Cloxacillin is an orally activeantibacterialagent andβ-lactamaseinhibitor with anIC50of 0.04 μM. Cloxacillin can suppress theS. aureus-induced inflammatory response by inhibiting the activation ofMAPKs,NF-кBandNLRP3-related proteins[1][2][3]. |
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体外研究
(In Vitro) | Cloxacillin (0-2048 μg/mL; 20-24 h) shows good antibacterial activity forS. aureus8325-4 and DU1090 with MIC values both of 0.125 μg/mL[1].
Cloxacillin (0.015625 μg/mL; 6 h) inhibits the hemolytic activity of Hlα in vitro, and this inhibition is not only more pronounced when combined with TZ and TZ, but also suppresses the inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins[1].
Cell Viability Assay[1] | Cell Line: | S. aureus8325-4,S. aureusDU1090 (an Hlα-deleted strain) | | Concentration: | 0-2048 μg/mL | | Incubation Time: | 20-24 h | | Result: | InhibitedS. aureus8325-4 and DU1090 with MIC values both of 0.125 μg/mL. |
Western Blot Analysis[1] | Cell Line: | S. aureus8325-4 | | Concentration: | 0.015625 μg/mL (combines with Thioridazine (TZ, 0.25 μg/mL) and Tetracycline (TC, 0.03125 μg/mL)). | | Incubation Time: | 6 h | | Result: | Inhibited the expression of Hlα and the inhibition was more pronounced when combined with TZ and TC. |
Western Blot Analysis[1] | Cell Line: | RAW264.7 cells (exposes toS. aureus8325-4/DU1090 or pure Hlα) | | Concentration: | 0.015625 μg/mL (combines with TZ (0.25 μg/mL) and TC (0.03125 μg/mL)). | | Incubation Time: | 6 h | | Result: | Inhibited the activation of MAPKs, NF-кB and NLRP3-related proteins thereby inhibiting the inflammatory response when combined with TC and TZ. |
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体内研究
(In Vivo) | Cloxacillin (1.6125 mg/kg; s.c.; 12-h intervals for 72 h) protects mice fromS. aureusperitonitis in vivo when combines with Thioridazine and Tetracycline[1].
Cloxacillin (7.5 mg/per; i.p.; twice daily from day 3 for 3 days) develops less severe synovitis and reduces bone erosions when combines with anti-IL-15 antibodies[3].
| Animal Model: | Female BALB/c mice (6-week-old; peritonitis model)[1]. | | Dosage: | 1.6125 mg/kg (combines with TC (3.125 mg/kg) and TZ (25 mg/kg)) | | Administration: | Subcutaneous injection; 12-h intervals for 72 h. | | Result: | Reduced the degree of inflammatory cell infiltration in the mouse lung tissue and alveolar structures tended to be normal.
Significantly reduced the pathological changes in spleen and liver tissue, as well as decreased the CFU counts ofS. aureusin the peritoneal cavity. |
| Animal Model: | Female wildtype C57BL/6 mice (8-week-old; systemicS. aureus-induced arthritis model) | | Dosage: | 7.5 mg/per (combines with 25 μg/per anti-IL-15 antibodies) | | Administration: | Intraperitoneal injection; twice daily from day 3 (after bacterial inoculation) and stopped at day 6. | | Result: | Showed activities of reducing severe synovitis and bone erosions when combined with anti-IL-15 antibodies. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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