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Product IntroductionBioactivity英文名: Valnemulin hydrochloride描述: Valnemulin hydrochloride (Valnemulin HCl) 是截短侧耳素抗生素，与 50s
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Product Introduction
Bioactivity
英文名: Valnemulin hydrochloride
描述: Valnemulin hydrochloride (Valnemulin HCl) 是截短侧耳素抗生素，与 50s 核糖体亚基中的肽基转移酶结合来抑制细菌中的蛋白质合成。
体外活性: Valnemulin (20 μM) completely inhibits the peptidyl transferase reaction, thus inhibits peptide bond formation. Valnemulin enhances the reactivity of nucleotides A2058 and A2059 moderately, whereas they protect U2506 strongly. [1] Valnemulin shows exceptional activity against M hyopneumoniae (MIC90 0.5 μg/mL) and M hyosynoviae (MIC range 0.1-0.25 0.5 μg/mL) field strains. [2] Valnemulin is mainly active against Gram-positive bacteria with moderate activity against some fastidious Gram-negative bacilli (e.g., anaerobic bacteria) and Mycoplasma and is used almost exclusively in animals, largely in swine in China. [3]
体内活性: Valnemulin is absorbed rapidly, distributed widely and rapidly and excreted rapidly after oral administration to rats. [3] Valnemulin results in a rapid diminution of clinical signs, restoration of appetite and reversal of weight loss in young calves. Valnemulin results in a more rapid reduction of clinical scores and eliminated M. bovis from the lungs more effectively than Enrofloxacin. [4] Valnemulin significantly decreases the wet-to-dry weight (W/D) ratios of lungs, protein concentrations, and the number of total cells, neutrophils, macrophages, and leukomonocytes, and histologic analysis indicates that valnemulin significantly attenuates tissue injury. Valnemulin significantly increases LPS-induced SOD activity in BALF and decreases lung myeloperoxidase (MPO) activity activity as well. Valnemulin also inhibits the production of tumor necrosis factor-alpha, interleukin-6, and interleukin-1beta, which is consistent with mRNA expression in lung. [5]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : 92 mg/mL (153 mM)
DMSO : 93 mg/mL (154.7 mM)
Ethanol : 93 mg/mL (154.7 mM)
关键字: Antibiotic | inhibit | Valnemulin hydrochloride | Valnemulin | Inhibitor | Bacterial | Valnemulin Hydrochloride
相关产品: Cefathiamidine | Antimycobacterial agent-4 | Virginiamycin M1 | G43 | FPI-1523 sodium | Amikacin hydrate | Nifuroxazide | Lanopepden mesylate | Clofoctol | 4-Hydroxybenzoic acid
相关库: Antibiotics Library | FDA-Approved & Pharmacopeia Drug Library | Macrocyclic Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Bacterial Compound Library | NO PAINS Compound Library | Anti-Infection Compound Library | Bioactive Compound Library
Bioactivity
英文名: Valnemulin hydrochloride
描述: Valnemulin hydrochloride (Valnemulin HCl) 是截短侧耳素抗生素，与 50s 核糖体亚基中的肽基转移酶结合来抑制细菌中的蛋白质合成。
体外活性: Valnemulin (20 μM) completely inhibits the peptidyl transferase reaction, thus inhibits peptide bond formation. Valnemulin enhances the reactivity of nucleotides A2058 and A2059 moderately, whereas they protect U2506 strongly. [1] Valnemulin shows exceptional activity against M hyopneumoniae (MIC90 0.5 μg/mL) and M hyosynoviae (MIC range 0.1-0.25 0.5 μg/mL) field strains. [2] Valnemulin is mainly active against Gram-positive bacteria with moderate activity against some fastidious Gram-negative bacilli (e.g., anaerobic bacteria) and Mycoplasma and is used almost exclusively in animals, largely in swine in China. [3]
体内活性: Valnemulin is absorbed rapidly, distributed widely and rapidly and excreted rapidly after oral administration to rats. [3] Valnemulin results in a rapid diminution of clinical signs, restoration of appetite and reversal of weight loss in young calves. Valnemulin results in a more rapid reduction of clinical scores and eliminated M. bovis from the lungs more effectively than Enrofloxacin. [4] Valnemulin significantly decreases the wet-to-dry weight (W/D) ratios of lungs, protein concentrations, and the number of total cells, neutrophils, macrophages, and leukomonocytes, and histologic analysis indicates that valnemulin significantly attenuates tissue injury. Valnemulin significantly increases LPS-induced SOD activity in BALF and decreases lung myeloperoxidase (MPO) activity activity as well. Valnemulin also inhibits the production of tumor necrosis factor-alpha, interleukin-6, and interleukin-1beta, which is consistent with mRNA expression in lung. [5]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : 92 mg/mL (153 mM)
DMSO : 93 mg/mL (154.7 mM)
Ethanol : 93 mg/mL (154.7 mM)
关键字: Antibiotic | inhibit | Valnemulin hydrochloride | Valnemulin | Inhibitor | Bacterial | Valnemulin Hydrochloride
相关产品: Cefathiamidine | Antimycobacterial agent-4 | Virginiamycin M1 | G43 | FPI-1523 sodium | Amikacin hydrate | Nifuroxazide | Lanopepden mesylate | Clofoctol | 4-Hydroxybenzoic acid
相关库: Antibiotics Library | FDA-Approved & Pharmacopeia Drug Library | Macrocyclic Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Bacterial Compound Library | NO PAINS Compound Library | Anti-Infection Compound Library | Bioactive Compound Library
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