Valnemulin HCl

Catalog No.S4216 Batch:S421601

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Technical Data

Formula

C31H52N2O5S.HCl

Molecular Weight 601.28 CAS No. 133868-46-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (166.31 mM)
Water 100 mg/mL (166.31 mM)
Ethanol 100 mg/mL (166.31 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Valnemulin HCl is a broad-spectrum bacteriostatic agent inhibiting protein synthesis in bacteria by binding to the peptidyl transferase component of the 50S subunit of ribosomes.
Targets
peptidyl transferase [1]
In vitro 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]
In vivo 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]

Protocol (from reference)

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.