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编 号:F406844
分子式:C19H18ClN3O5S
分子量:435.88
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Cloxacillin is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 μM. Cloxacillin can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins.

体内研究:
Cloxacillin (1.6125 mg/kg; s.c.; 12-h intervals for 72 h) protects mice from S. aureus peritonitis in vivo when combines with Thioridazine and Tetracycline.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.Animal Model:Female BALB/c mice (6-week-old; peritonitis model).
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 of S. aureus in the peritoneal cavity.
Animal Model:Female wildtype C57BL/6 mice (8-week-old; systemic S. 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.

体外研究:
Cloxacillin (0-2048 μg/mL; 20-24 h) shows good antibacterial activity for S. aureus 8325-4 and DU1090 with MIC values both of 0.125 μg/mL.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.
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