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编 号:F339600
分子式:C80H106Cl2N11O27P
分子量:1755.63
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生物活性:
Telavancin (TD-6424) is a semisynthetic lipoglycopeptide vancomycin-derivative, is a novel antimicrobial agent developed by Theravance for overcoming resistant Gram-positive bacterial infections, specifically methicillin-resistant Staphylococcus aureus (MRSA). Telavancin disrupts cell membrane integrity, can be used for research of complicated skin and skin structure infections (cSSSIs) caused by Gram-positive bacteria.

体内研究:
Telavancin has been tested in various relevant animal models of infection, namely, bacteremia (40 mg/kg/d; s.c.; twice a day, with 12 h space), endocarditis (30 mg/kg/d; i.v.; twice a day, with 12 h space; 4 d), meningitis, and pneumonia with successAnimal Model:MRSA bacteremia model in neutropenic mice
Dosage:40 mg/kg
Administration:Subcutaneous injection; twice every day spaced 12 h apart?
Result:Resulted a significantly higher 14-day survival compared with vancomycin-treated animals.
Animal Model:Rabbit model of S. aureus endocarditis
Dosage:30 mg/kg
Administration:Intravenous injection; twice every day, spaced 12 h for 4 days
Result:Significantly reduced MRSA densities in all target tissues and increased the percentage of these organs rendered culture negative.

体外研究:
Telavancin has a rapid, concentration-dependent bactericidal effect, due to disruption of cell membrane integrity.Telavancin (5 μg/mL) exerts bacteriocidal effect against a MRSA strain (COL) and a VISA strain (HIP5836) at a concentration of 5 μg/mL.
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