| Size | Price | |
|---|---|---|
| 50mg | ||
| 100mg | ||
| 250mg | ||
| Other Sizes |
| Targets |
The primary target of Spiramycin III is the bacterial 50S ribosomal subunit. It inhibits protein synthesis by blocking the translocation step of translation. It binds to the 50S subunit with an apparent 1:1 stoichiometry. This binding inhibits the interaction of the ribosome with aminoacyl-tRNA and prevents peptide bond formation. The compound is active against a range of Gram-positive bacteria and some Gram-negative bacteria, as well as Toxoplasma gondii.
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|---|---|
| ln Vitro |
In vitro, Spiramycin III inhibits the binding of tetrahydroleucomycin A3 to E. coli ribosomes with an IC50 of 1 µM. It is active against Staphylococcus aureus, Bacillus subtilis, Bacillus cereus, and Micrococcus luteus with MIC values ranging from 0.1 to 3.12 µg/mL. It inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit. Specific MIC values against various bacterial strains are reported in the literature.
|
| ln Vivo |
In vivo, Spiramycin III is used clinically to treat toxoplasmosis and various infections of soft tissues. It is administered orally and is effective against susceptible bacterial infections and toxoplasmosis. The compound is also used in veterinary medicine. Specific published in vivo efficacy data, including dosing regimens and outcome measures, are reported in clinical and preclinical literature.
|
| Enzyme Assay |
The ribosomal binding assay uses purified E. coli ribosomes or 50S subunits. Radiolabeled tetrahydroleucomycin A3 or a fluorescent macrolide probe is incubated with ribosomes and Spiramycin III at serial dilutions. Bound radioactivity or fluorescence is separated by filtration and quantified. IC50 values are calculated from competition curves. The assay is used to characterize macrolide binding to the 50S subunit.
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| Cell Assay |
For cell-based assays, bacterial strains are cultured and treated with serial dilutions of Spiramycin III. After incubation at 37°C for 18-24 hours, growth inhibition is measured by optical density. MIC values are determined according to CLSI guidelines. For Toxoplasma gondii assays, infected host cells are treated with the compound, and parasite replication is measured by qPCR or microscopy.
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| Animal Protocol |
In vivo studies with Spiramycin III employ rodent models of bacterial infection or toxoplasmosis. The compound is dissolved in saline or appropriate vehicle and administered orally or intraperitoneally. Doses are selected based on MIC values and pharmacokinetic studies. Key readouts include survival rates, bacterial burden in tissues, and parasite load. Tissues are harvested for histopathological analysis.
|
| References |
|
| Molecular Formula |
C46H78N2O15
|
|---|---|
| Molecular Weight |
899.12
|
| Exact Mass |
898.54
|
| CAS # |
24916-52-7
|
| Related CAS # |
8025-81-8;24916-52-7 (III);67724-08-7 (Embonate);68880-55-7 (adipate);
|
| PubChem CID |
5284621
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.2g/cm3
|
| Boiling Point |
923.6ºC at 760mmHg
|
| Flash Point |
512.4ºC
|
| Vapour Pressure |
0mmHg at 25°C
|
| Index of Refraction |
1.542
|
| Source |
Originated from microorganisms: Escherichia coli.
|
| LogP |
3.286
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
17
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
63
|
| Complexity |
1500
|
| Defined Atom Stereocenter Count |
19
|
| SMILES |
O=CC[C@H]1C[C@@H](C)[C@@H](O[C@H]2CC[C@H](N(C)C)[C@@H](C)O2)C=CC=CC[C@@H](C)OC(=O)C[C@@H](OC(CC)=O)[C@H](OC)[C@H]1O[C@@H]1O[C@H](C)[C@@H](O[C@@H]2O[C@@H](C)[C@H](O)[C@](C)(O)C2)[C@H](N(C)C)[C@H]1O |c:22,t:20,&1:3,5,7,9,12,16,24,30,36,39,41,43,45,47,49,51,53,57,61|
|
| InChi Key |
HSZLKTCKAYXVBX-HHTHJJQKSA-N
|
| InChi Code |
InChI=1S/C46H78N2O15/c1-13-35(50)60-34-24-36(51)56-27(3)17-15-14-16-18-33(61-37-20-19-32(47(8)9)28(4)57-37)26(2)23-31(21-22-49)42(43(34)55-12)63-45-40(52)39(48(10)11)41(29(5)59-45)62-38-25-46(7,54)44(53)30(6)58-38/h14-16,18,22,26-34,37-45,52-54H,13,17,19-21,23-25H2,1-12H3/b15-14+,18-16+/t26-,27-,28-,29-,30+,31+,32+,33+,34-,37-,38+,39-,40-,41-,42+,43+,44+,45+,46-/m1/s1
|
| 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-[(2S,5S,6R)-5-(dimethylamino)-6-methyloxan-2-yl]oxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)-1-oxacyclohexadeca-11,13-dien-4-yl] propanoate
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1122 mL | 5.5610 mL | 11.1220 mL | |
| 5 mM | 0.2224 mL | 1.1122 mL | 2.2244 mL | |
| 10 mM | 0.1112 mL | 0.5561 mL | 1.1122 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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