Home Microbiology Bacterial chemical Valnemulin HCl

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Valnemulin HCl Bacterial chemical

Cat.No.S4216

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.
Valnemulin HCl Bacterial chemical Chemical Structure

Chemical Structure

Molecular Weight: 601.28

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Quality Control

Batch: S421601 DMSO]100 mg/mL]false]Water]100 mg/mL]false]Ethanol]100 mg/mL]false Purity: 99.62%
99.62

Chemical Information, Storage & Stability

Molecular Weight 601.28 Formula

C31H52N2O5S.HCl

 Storage (From the date of receipt)
CAS No. 133868-46-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1CCC23CCC(=O)C2C1(C(CC(C(C3C)O)(C)C=C)OC(=O)CSC(C)(C)CNC(=O)C(C(C)C)N)C.Cl

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (166.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
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]
References

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