| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Lincomycin hydrochloride targets the bacterial ribosome, specifically the 23S rRNA of the 50S ribosomal subunit. By binding to this site, it inhibits the transpeptidase reaction and prevents peptide bond formation, thereby inhibiting protein synthesis. This mechanism is bacteriostatic for most susceptible organisms. The hydrochloride salt form improves the compound's solubility and stability.
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|---|---|
| ln Vitro |
In vitro, lincomycin hydrochloride demonstrates activity against Gram-positive bacteria, including various strains of S. aureus and Streptococcus species. Its minimum inhibitory concentrations (MICs) against susceptible strains are well-documented. It is a narrow-spectrum antibiotic with similar potency to erythromycin.
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| ln Vivo |
The frequency of stimulation in rabbit sciatic nerve gastrocnemius muscle preparations determines how much lincomycin (25 and 50 mg/kg, intravenously) inhibits neuromuscular transmission [3].
In vivo, lincomycin hydrochloride is used to treat infections caused by Staphylococcus aureus, Streptococcus species, and Bacteroides fragilis. It is also used in veterinary medicine for joint and respiratory infections. Its clinical efficacy is well-established for these indications. |
| Enzyme Assay |
Non-cell-based assays for lincomycin hydrochloride are not typical, as its mechanism of action involves binding to the ribosome. However, its activity can be assessed in cell-free translation systems.
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| Cell Assay |
Cellular assays for lincomycin hydrochloride are performed using standard broth microdilution or agar dilution methods to determine the minimum inhibitory concentration (MIC) against bacterial strains. Bacteria are cultured in appropriate medium and treated with lincomycin at various concentrations. Bacterial growth is assessed by optical density measurement or colony counting after overnight incubation.
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| Animal Protocol |
Animal/Disease Models: Adult albino New Zealand rabbit, weighing 2.5-3.5 kg [3].
Doses: 25 and 50 mg/kg. Mode of Route of Administration: intravenous (iv) (iv)injection Experimental Results: Neuromuscular transmission is inhibited. In vivo animal models for lincomycin hydrochloride would typically involve the use of mice infected with a pathogenic bacterium. The compound is administered, and its efficacy is assessed by measuring survival rates and bacterial burden. |
| ADME/Pharmacokinetics |
Lincomycin hydrochloride monohydrate has a molecular weight of 461.01 g/mol and a molecular formula of C18H35ClN2O7S. It is soluble in water. It is typically administered orally or parenterally. Detailed PK parameters such as half-life and bioavailability are well-established from clinical use but are not extensively detailed in the provided search results.
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| Toxicity/Toxicokinetics |
Lincomycin hydrochloride has a well-established safety profile from its clinical use. Common side effects include gastrointestinal disturbances, such as diarrhea and nausea. Pseudomembranous colitis is a serious potential adverse effect. The compound is intended for research use only and is not for human consumption in a research context.
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| References |
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| Additional Infomation |
Lincomycin hydrochloride is the hydrochloride form of lincomycin, a lincosamide antibiotic originally discovered from the actinomycete Streptomyces lincolnensis. It is active against Gram-positive cocci and anaerobic bacteria. It is an antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used to treat infections caused by Staphylococcus, Streptococcus, and Bacteroides fragilis.
Lincomycin hydrochloride is the hydrochloride salt of lincomycin. It is a narrow-spectrum antibiotic effective against Gram-positive bacteria. It binds to the 23S rRNA of the 50S ribosomal subunit and inhibits protein synthesis. It is used for the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections. It has the CAS number 7179-49-9 and is supplied for research purposes. |
| Molecular Formula |
C18H37CLN2O7S
|
|---|---|
| Molecular Weight |
461.01
|
| Exact Mass |
460.2
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| CAS # |
7179-49-9
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| Related CAS # |
Lincomycin;154-21-2;Lincomycin hydrochloride;859-18-7
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| PubChem CID |
71476
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| Appearance |
White to off-white solid powder
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| Boiling Point |
646.8ºC at 760 mmHg
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| Melting Point |
154 °C
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| Flash Point |
345ºC
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| LogP |
0.209
|
| Hydrogen Bond Donor Count |
7
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
29
|
| Complexity |
499
|
| Defined Atom Stereocenter Count |
9
|
| SMILES |
CCC[C@@H]1C[C@H](N(C1)C)C(=O)N[C@@H]([C@@H]2[C@@H]([C@@H]([C@H]([C@H](O2)SC)O)O)O)[C@@H](C)O.O.Cl
|
| InChi Key |
LFZGYTBWUHCAKF-DCNJEFSFSA-N
|
| InChi Code |
InChI=1S/C18H34N2O6S.ClH.H2O/c1-5-6-10-7-11(20(3)8-10)17(25)19-12(9(2)21)16-14(23)13(22)15(24)18(26-16)27-4;;/h9-16,18,21-24H,5-8H2,1-4H3,(H,19,25);1H;1H2/t9-,10-,11+,12-,13+,14-,15-,16-,18-;;/m1../s1
|
| Chemical Name |
(2S,4R)-N-[(1R,2R)-2-hydroxy-1-[(2R,3R,4S,5R,6R)-3,4,5-trihydroxy-6-methylsulfanyloxan-2-yl]propyl]-1-methyl-4-propylpyrrolidine-2-carboxamide;hydrate;hydrochloride
|
| Synonyms |
Lincomycin HCl; Lincomix; Lincocin
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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)
|
| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~216.92 mM)
H2O : ~50 mg/mL (~108.46 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.42 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 (5.42 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 (5.42 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: 120 mg/mL (260.30 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 | 2.1692 mL | 10.8458 mL | 21.6915 mL | |
| 5 mM | 0.4338 mL | 2.1692 mL | 4.3383 mL | |
| 10 mM | 0.2169 mL | 1.0846 mL | 2.1692 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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