| Size | Price | Stock | Qty |
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| 2g |
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| 5g |
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| 10g |
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| Other Sizes |
| Targets |
Acetylspiramycin targets the 50S ribosomal subunit of the bacterial ribosome. By binding to this subunit, it inhibits bacterial protein synthesis. This is its primary mechanism of action. It also inhibits splenic lymphocyte transformation.
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|---|---|
| ln Vitro |
In cell-free systems, Acetylspiramycin's activity is assessed by its ability to inhibit protein synthesis. This can be measured using an in vitro translation system where the compound's effect on the incorporation of labeled amino acids into protein is quantified. In vitro, Acetylspiramycin exhibits potent antibacterial activity against Gram-positive bacteria, including Streptococcus pyogenes, S. viridans, Corynebacterium diphtheriae, and methicillin-sensitive Staphylococcus aureus. It also inhibits lymphocyte transformation induced by PHA and LPS.
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| ln Vivo |
In vivo, Acetylspiramycin is an effective oral macrolide antibiotic. It is used to treat bacterial infections in clinical and preclinical settings. Its efficacy has been demonstrated in various animal models of infection.
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| Enzyme Assay |
The antibacterial activity of Acetylspiramycin is tested in vitro using standardized susceptibility testing methods, such as broth microdilution or agar diffusion. The minimum inhibitory concentration (MIC) is determined against a panel of bacterial strains.
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| Cell Assay |
Cell-based assays are used to study its effect on immune cells. For example, its inhibition of lymphocyte transformation is assessed by stimulating splenic lymphocytes with PHA or LPS and measuring proliferation in the presence of the compound.
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| Animal Protocol |
In vivo efficacy is evaluated in animal models of bacterial infection. Animals are infected with a pathogenic bacterium and then treated with Acetylspiramycin. The reduction in bacterial load and survival rate are measured.
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| ADME/Pharmacokinetics |
Acetylspiramycin is orally bioavailable. Its improved bioavailability and stability compared to spiramycin make it a valuable antibiotic. It is metabolized in the liver and excreted in bile and urine. Its half-life allows for convenient dosing.
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| Toxicity/Toxicokinetics |
Acetylspiramycin is generally well-tolerated. Side effects are similar to other macrolides and may include gastrointestinal disturbances. It is contraindicated in patients with known hypersensitivity to macrolide antibiotics. It is approved for clinical use in some countries.
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| References | |
| Additional Infomation |
Spiramycin II is a cyclic macrolide antibiotic produced by various Streptomyces species. It has dual action as an antibacterial agent, antimicrobial agent, and bacterial metabolite. Its structure includes aldehydes, disaccharide derivatives, ethers, cyclic macrolides, tertiary amine compounds, and acetates. Spiramycin II has been reported to exist in Streptomyces ambroxolus, and relevant data are available for reference.
Acetylspiramycin is a macrolide antibiotic used to treat bacterial infections. It is a valuable tool for studying bacterial protein synthesis and antimicrobial resistance. It is available as a pharmaceutical product in some regions. |
| Molecular Formula |
C45H76N2O15
|
|---|---|
| Molecular Weight |
885.0894
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| Exact Mass |
884.524
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| CAS # |
24916-51-6
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| PubChem CID |
5282173
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
916.7±65.0 °C at 760 mmHg
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| Melting Point |
130-133ºC
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| Flash Point |
508.2±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.543
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
62
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| Complexity |
1480
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| Defined Atom Stereocenter Count |
19
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| SMILES |
O1[C@]([H])(C([H])([H])[H])[C@]([H])([C@@]([H])([C@]([H])([C@]1([H])O[C@]1([H])[C@]([H])([C@@]([H])(C([H])([H])C(=O)O[C@]([H])(C([H])([H])[H])C([H])([H])C([H])=C([H])C([H])=C([H])[C@@]([H])([C@]([H])(C([H])([H])[H])C([H])([H])[C@]1([H])C([H])([H])C([H])=O)O[C@]1([H])C([H])([H])C([H])([H])[C@@]([H])([C@@]([H])(C([H])([H])[H])O1)N(C([H])([H])[H])C([H])([H])[H])OC(C([H])([H])[H])=O)OC([H])([H])[H])O[H])N(C([H])([H])[H])C([H])([H])[H])O[C@@]1([H])C([H])([H])[C@](C([H])([H])[H])([C@]([H])([C@]([H])(C([H])([H])[H])O1)O[H])O[H] |c:39,43|
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| InChi Key |
ZPCCSZFPOXBNDL-RSMXASMKSA-N
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| InChi Code |
InChI=1S/C45H76N2O15/c1-25-22-31(20-21-48)41(62-44-39(51)38(47(10)11)40(28(4)58-44)61-37-24-45(7,53)43(52)29(5)57-37)42(54-12)34(59-30(6)49)23-35(50)55-26(2)16-14-13-15-17-33(25)60-36-19-18-32(46(8)9)27(3)56-36/h13-15,17,21,25-29,31-34,36-44,51-53H,16,18-20,22-24H2,1-12H3/b14-13+,17-15+/t25-,26-,27+,28-,29+,31+,32+,33+,34-,36+,37+,38-,39-,40-,41+,42+,43+,44+,45-/m1/s1
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| Chemical Name |
[(4R,5S,6S,7R,9R,10R,11E,13E,16R)-6-[(2S,3R,4R,5S,6R)-5-[(2S,4R,5S,6S)-4,5-dihydroxy-4,6-dimethyloxan-2-yl]oxy-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-10-[(2R,5S,6S)-5-(dimethylamino)-6-methyloxan-2-yl]oxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)-1-oxacyclohexadeca-11,13-dien-4-yl] acetate
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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 |
| 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) |
DMSO : ≥ 50 mg/mL (~56.49 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.82 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 (2.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1298 mL | 5.6491 mL | 11.2983 mL | |
| 5 mM | 0.2260 mL | 1.1298 mL | 2.2597 mL | |
| 10 mM | 0.1130 mL | 0.5649 mL | 1.1298 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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