| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Macrolide
50S ribosomal subunit (bacterial). |
|---|---|
| ln Vitro |
Erythromycin is used to treat infections of the skin and soft tissues in addition to gastrointestinal, genital, and respiratory tract infections. Since the first generation of macrolides, which had low toxicity and good tolerability, are unstable in acidic media, erythromycin, with its ten chiral centers and two sugar substituents (L-cladinose and D-desosamine), is a good starting point for numerous medicinal chemistry efforts to improve its biological profile (better activity, higher stability, and improved bioavailability[1].
Davercin binds to the 50S ribosomal subunit and inhibits bacterial protein synthesis. It blocks the progression of nascent polypeptide chains, thereby preventing bacterial growth. It has broad-spectrum activity against various Gram-positive and Gram-negative bacteria, with MICs ranging from 0.02-50 μg/ml. |
| ln Vivo |
Macrolides, as a class of natural or semisynthetic products, express their antibacterial activity primarily by reversible binding to the bacterial 50S ribosomal subunits and by blocking nascent proteins' progression through their exit tunnel in bacterial protein biosynthesis. Generally considered to be bacteriostatic, they may also be bactericidal at higher doses. The discovery of azithromycin from the class of macrolides, as one of the most important new drugs of the 20th century, is presented as an example of a rational medicinal chemistry approach to drug design, applying classical structure-activity relationship that will illustrate an impressive drug discovery success story. However, the microorganisms have developed several mechanisms to acquire resistance to antibiotics, including macrolide antibiotics. The primary mechanism for acquiring bacterial resistance to macrolides is a mutation of one or more nucleotides from the binding site. Although azithromycin is reported to show different, two-step process of the inhibition of ribosome function of some species, more detailed elaboration of that specific mode of action is needed. New macrocyclic derivatives, which could be more potent and less prone to escape bacterial resistance mechanisms, are also continuously evaluated. A novel class of antibiotic compounds-macrolones, which are derived from macrolides and comprise macrocyclic moiety, linker, and either free or esterified quinolone 3-carboxylic group, show excellent antibacterial potency towards key erythromycin-resistant Gram-positive and Gram-negative bacterial strains, with possibly decreased potential of bacterial resistance to macrolides[1].
In vivo, Davercin has been studied for its efficacy in treating bacterial infections in animal models. As a macrolide antibiotic, it is expected to have good tissue penetration and activity against susceptible bacterial strains. It has been used in the treatment of respiratory, gastrointestinal, and genital tract infections. |
| Enzyme Assay |
Davercin is evaluated in cell-free assays using bacterial ribosomes. The compound is incubated with ribosomes and a substrate, and the inhibition of protein synthesis is measured. IC50 values are determined to quantify the potency of protein synthesis inhibition.
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| Cell Assay |
No detailed cell assay protocols available for Davercin specifically. As a macrolide antibiotic, it is typically evaluated in bacterial culture assays to determine minimum inhibitory concentrations (MICs) against various bacterial strains. Bacteria are grown in broth or agar media containing varying concentrations of Davercin, and growth inhibition is measured.
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| Animal Protocol |
No detailed animal protocol available. Davercin has been studied in animal models of bacterial infection, where efficacy is assessed by measuring bacterial load reduction and survival rates.
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| ADME/Pharmacokinetics |
Davercin (Erythromycin cyclocarbonate) has a molecular formula of C38H65NO14 and molecular weight of 759.92. Soluble in DMF, DMSO, and ethanol. Storage at -20°C.
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| Toxicity/Toxicokinetics |
No detailed toxicity data available. As a macrolide antibiotic, it is expected to have a safety profile similar to erythromycin, with potential gastrointestinal side effects.
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| References | |
| Additional Infomation |
Davercin is an aminoglycoside antibiotic.
Davercin (Erythromycin cyclocarbonate) is a macrolide antibiotic. It is a derivative of Erythromycin. Molecular formula: C38H65NO14; MW: 759.92. Purity ≥98%. Used in the treatment of bacterial infections. |
| Molecular Formula |
C38H65NO14
|
|---|---|
| Molecular Weight |
759.9210
|
| Exact Mass |
759.441
|
| Elemental Analysis |
C, 60.06; H, 8.62; N, 1.84; O, 29.47
|
| CAS # |
55224-05-0
|
| Related CAS # |
114-07-8 (free); 3521-62-8 (estolate); 16667-03-1 (glutamate); 30010-41-4 (aspartate); 7704-67-8 (thiocyante); 1264-62-6 (Ethylsuccinate); 914076-30-5 (ethyl carbonate); 55224-05-0 (cyclocarbonate); 33396-29-1 (Erythromycin A enol ether); 59319-72-1 (Erythromycin A dihydrate) |
| PubChem CID |
10033072
|
| Appearance |
White to off-white solid powder; Colorless solution (in ethanol, 100mg/mL)
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| Density |
1.22 g/cm3
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| Boiling Point |
859.8ºC at 760 mmHg
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| Index of Refraction |
1.534
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| LogP |
2.967
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
53
|
| Complexity |
1300
|
| Defined Atom Stereocenter Count |
18
|
| SMILES |
O([C@@]1([H])[C@@]([H])([C@]([H])(C([H])([H])[C@@]([H])(C([H])([H])[H])O1)N(C([H])([H])[H])C([H])([H])[H])O[H])[C@@]1([H])[C@@](C([H])([H])[H])(C([H])([H])[C@@]([H])(C([H])([H])[H])C([C@]([H])(C([H])([H])[H])[C@]2([H])[C@@](C([H])([H])[H])([C@@]([H])(C([H])([H])C([H])([H])[H])OC([C@]([H])(C([H])([H])[H])[C@]([H])([C@]1([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])OC([H])([H])[H])=O)OC(=O)O2)=O)O[H]
|
| InChi Key |
NKLGIWNNVDPGCA-ZDYKNUMJSA-N
|
| InChi Code |
InChI=1S/C38H65NO14/c1-14-25-38(10)32(52-35(44)53-38)20(4)27(40)18(2)16-36(8,45)31(51-34-28(41)24(39(11)12)15-19(3)47-34)21(5)29(22(6)33(43)49-25)50-26-17-37(9,46-13)30(42)23(7)48-26/h18-26,28-32,34,41-42,45H,14-17H2,1-13H3/t18-,19-,20+,21+,22-,23+,24+,25-,26+,28-,29+,30+,31-,32-,34+,36-,37-,38-/m1/s1
|
| Chemical Name |
(3aR,4R,7R,8S,9S,10R,11R,13R,15R,15aR)-10-(((2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-4-ethyl-11-hydroxy-8-(((2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl)oxy)-3a,7,9,11,13,15-hexamethyldecahydro-6H-[1,3]dioxolo[4,5-c][1]oxacyclotetradecine-2,6,14(7H)-trione
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| Synonyms |
Erythromycin A; Erythromycin A 11,12-carbonate; Erythromycin A cyclic carbonate; Davercin;
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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 : 100 mg/mL (131.59 mM)
Ethanol : 100 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (3.95 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 30.0 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: ≥ 3 mg/mL (3.95 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 30.0 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: ≥ 3 mg/mL (3.95 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: ≥ 3 mg/mL (3.95 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3159 mL | 6.5796 mL | 13.1593 mL | |
| 5 mM | 0.2632 mL | 1.3159 mL | 2.6319 mL | |
| 10 mM | 0.1316 mL | 0.6580 mL | 1.3159 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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