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Delpazolid

CAS No. : 1219707-39-7

MCE 站：Delpazolid

产品活性：Delpazolid 是一种新型的恶唑烷酮类抗生素，能抑制 MSSA 和 MRSA 的生长，对它们的 MIC₉₀ 值都为 2 μg/mL。

研究领域：Anti-infection

作用靶点：Bacterial  |  Antibiotic

In Vitro: Delpazolid (LCB01-0371), at concentrations of 1×MIC and 2×MIC, has bacteriostatic activity against MSSA and MRSA after 24 h. At concentrations of 4×MIC and 8×MIC, Delpazolid shows bacteriostatic activity, but there is no regrowth at concentrations of 4×MIC and 8×MIC after 24 h of incubation. The survival of M. abscessus is greatly decreased in the presence of Delpazolid (LCB-0371) (MIC₅₀=1.2 μg/mL). Delpazolid dramatically decreases the number of intracellular mycobacteria present at 2 days after infection at concentrations of 0.1, 1, and 10 μg/mL.

In Vivo: When administered orally, Delpazolid (LCB01-0371) shows potent protective effects against systemic infections caused by Gram-positive and Gram-negative bacteria. Against infection caused by S. aureus Giorgio (MSSA), the ED₅₀ of Delpazolid is 4.53 mg/kg of body weight. Against S. aureus p125 (MRSA), the ED₅₀ of Delpazolid is 2.96 mg/kg. When Delpazolid (LCB-0371) is administered at 100 mg/kg daily (by gavage), the colony-forming unit (CFU) counts tend to be decreased in the lungs of mice at 7 days after infection.

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