| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Valnemulin HCl, the hydrochloride salt of Valnemulin, is a pleuromutilin antibiotic with a wide-spectrum of antibiotic/antibacterial activity against mycoplasma and spirochete. It has been used for gastrointestinal disorders, and acts as a protein synthesis inhibitor. Valnemulin is commonly used as a veterinary drug. It can prevent and control swine dysentery, ileitis, colitis and other intestinal diseases, as well as swine asthma and other respiratory diseases.
| Targets |
Valnemulin targets the peptidyl transferase enzyme within the 50S ribosomal subunit, specifically binding to domain V of the 23S rRNA. This prevents accurate positioning of the CCA-end of tRNA by transpeptidase, thereby blocking peptide bond formation.
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| ln Vitro |
In cell-free assays, valnemulin (20 μM) completely inhibits the peptidyl transferase reaction, preventing peptide bond formation. It moderately enhances the reactivity of nucleotides A2058 and A2059 while strongly protecting U2506. Antimicrobial activity: MIC90 of 0.5 μg/mL against M. hyopneumoniae, MIC range 0.1–0.25 μg/mL against M. hyosynoviae, MIC of 0.125 μg/mL against S. aureus, and MIC of 0.063 μg/mL against C. perfringens.
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| Enzyme Assay |
In a cell-free system, valnemulin HCl (20 μM) is incubated with a reaction mixture containing ribosomal peptidyl transferase. Inhibition activity is assessed by detecting peptide bond formation products (e.g., puromycin reaction). Nucleotide reactivity of 23S rRNA (A2058, A2059, U2506) is determined using primer extension analysis or nucleotide chemical modification assays.
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| Cell Assay |
MIC determination is performed using broth microdilution or agar dilution methods following CLSI guidelines. Bacterial strains are inoculated into MHB or Mycoplasma-specific medium with serially diluted valnemulin HCl (e.g., 0.00625–12.8 μg/mL) and incubated at 35–37°C for 18–24 h. The MIC is read as the lowest concentration showing no visible bacterial growth. For S. aureus, a spectrophotometric method (OD at 630 nm) with a standard curve can also be used to assess antibacterial effects.
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| Animal Protocol |
(1) Chicken Mycoplasma gallisepticum infection model: Intratracheal M. gallisepticum inoculation establishes infection. Intramuscular administration of valnemulin HCl (1, 10, 20 mg/kg) with LC-MS/MS for PK analysis and RT-PCR for bacterial quantification; AUC24/MIC ratio is used to evaluate efficacy.；(2) Swine dysentery model: Oral challenge with Brachyspira hyodysenteriae in pigs, followed by in-feed valnemulin HCl (e.g., 75 mg/kg feed). Efficacy is assessed via fecal shedding counts, colonic mucosal morphology, and clinical scores.；(3) Mouse acute lung injury model: Intratracheal LPS instillation in BALB/c mice induces ALI; oral gavage of valnemulin HCl (100 mg/kg, single dose); inflammatory cell and cytokine levels in BALF are measured.
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| ADME/Pharmacokinetics |
In pigs, valnemulin is rapidly absorbed after oral administration with an absorption rate >90%. Tmax is 1–4 h, terminal plasma half-life is 1.3–2.7 h, and oral bioavailability is approximately 83–90%. At 10 mg/kg oral dose, Cmax is ~1.29 μg/mL and AUC is 5.58 μg·h/mL; plasma concentration is linearly related to dose. Valnemulin is widely distributed, with significantly higher drug concentrations in lung and liver than in plasma. Approximately 87% of the drug is metabolized in the liver, with metabolites primarily excreted via bile and feces (~87% within 3 days), while only ~3% is excreted renally. Rapid elimination from tissues is observed, and a withdrawal period of approximately 2 days is recommended.
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| Toxicity/Toxicokinetics |
Acute toxicity: Oral LD50 is 1374.4 mg/kg in mice and 1611.6 mg/kg in rats, classified as low toxicity. Repeat-dose toxicity: In rats receiving oral valnemulin for 13 weeks, liver injury and thyroid follicular epithelial hyperplasia were observed at 200 g/kg. Special toxicity studies indicate no reproductive toxicity, teratogenicity, mutagenicity, or carcinogenicity, with no effects on the immune system. Target animal safety: No significant toxic reactions were observed in pigs fed 75 mg/kg in feed for 28 consecutive days. GHS classification: Harmful if swallowed (Category 4), causes serious eye irritation (Category 2), may cause respiratory irritation (Category 3), and is very toxic to aquatic life with long-lasting effects (Acute Category 1 / Chronic Category 1).
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| References | |
| Additional Infomation |
See also: Valnemulin (contains active ingredient).
Drug Indications Swine: Treatment and prevention of swine dysentery. Treatment of clinical symptoms of swine proliferative enteropathy (ileitis). Prevention of clinical symptoms of confirmed swine spirochetal disease (colitis) in swine herds. Treatment and prevention of swine endemic pneumonia. The recommended dose is 10-12 mg/kg body weight, which can reduce lung lesions and weight loss, but cannot eradicate Mycoplasma hyopneumoniae infection. Rabbits: Reduction of mortality during outbreaks of rabbit epidemic enteropathy (ERE). Treatment should begin early in the outbreak, i.e., when the first rabbit is clinically diagnosed with the disease. |
| Molecular Formula |
C31H53CLN2O5S
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|---|---|
| Molecular Weight |
601.284
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| Exact Mass |
600.336
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| Elemental Analysis |
C, 61.92; H, 8.88; Cl, 5.90; N, 4.66; O, 13.30; S, 5.33
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| CAS # |
133868-46-9
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| Related CAS # |
101312-92-9;133868-46-9 (HCl);
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| PubChem CID |
60195218
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| Appearance |
White to off-white solid powder
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| Boiling Point |
672.7ºC at 760 mmHg
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| Flash Point |
360.6ºC
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| LogP |
6.397
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
40
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| Complexity |
969
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C[C@@H]([C@@H]([C@@](C)(C[C@H]1OC(CSC(C)(C)CNC([C@H](N)C(C)C)=O)=O)C=C)O)C(CCC2=O)(CC[C@H]3C)[C@]2([H])C31C.Cl
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| InChi Key |
MFBPRQKHDIVLOJ-AFFLPQGKSA-N
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| InChi Code |
InChI=1S/C31H52N2O5S.ClH/c1-10-29(8)15-22(38-23(35)16-39-28(6,7)17-33-27(37)24(32)18(2)3)30(9)19(4)11-13-31(20(5)26(29)36)14-12-21(34)25(30)31;/h10,18-20,22,24-26,36H,1,11-17,32H2,2-9H3,(H,33,37);1H/t19-,20+,22-,24-,25+,26+,29-,30+,31+;/m1./s1
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| Chemical Name |
[(1S,2R,3S,4S,6R,7R,8R,14R)-4-ethenyl-3-hydroxy-2,4,7,14-tetramethyl-9-oxo-6-tricyclo[5.4.3.01,8]tetradecanyl] 2-[1-[[(2R)-2-amino-3-methylbutanoyl]amino]-2-methylpropan-2-yl]sulfanylacetate;hydrochloride
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| Synonyms |
Valnemulin hydrochlordie; Valnemulin HCl; Econor;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~166.31 mM)
Ethanol : ~100 mg/mL DMSO : ~ 100 mg/mL (~166.31 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.16 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (4.16 mM) Solubility in Formulation 5: 100 mg/mL (166.31 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6631 mL | 8.3156 mL | 16.6312 mL | |
| 5 mM | 0.3326 mL | 1.6631 mL | 3.3262 mL | |
| 10 mM | 0.1663 mL | 0.8316 mL | 1.6631 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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