| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Not applicable. Descladinose 6-N-desmethyl azithromycin is a degradation product and impurity of azithromycin. It does not possess significant antibacterial activity compared to the parent drug. Azithromycin targets the bacterial 50S ribosomal subunit, inhibiting protein synthesis. This impurity has a modified sugar structure, which significantly reduces its binding affinity to the ribosome. It is not used as an antibiotic. Its role is to serve as a marker for the stability and purity of azithromycin formulations.
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|---|---|
| ln Vitro |
In vitro, this compound is not used for biological activity. It is an analytical standard. In an HPLC method for azithromycin, a system suitability solution containing azithromycin (2 mg/mL) and the impurity at 0.5-1.0 ug/mL is prepared. A C18 column (4.6 × 150 mm) is used with a mobile phase of acetonitrile:0.1 M ammonium acetate pH 6.5 (60:40). Detection is by evaporative light scattering (ELSD) or UV at 210 nm. The impurity is used to verify the resolution of the method. It has no direct antimicrobial activity in standard MIC assays against S. aureus or S. pneumoniae.
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| ln Vivo |
In vivo, this compound is not administered as a drug. It is a metabolite and impurity. When azithromycin is administered to animals, this impurity can be detected in plasma. It is monitored in pharmacokinetic studies to characterize the metabolic profile. It is not used for efficacy. In stability studies, azithromycin samples are stressed (heat, humidity, light), and this impurity is analyzed to ensure it remains below acceptable limits.
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| Enzyme Assay |
General protocol for in vitro analytical use: For HPLC analysis of Azithromycin impurities, prepare a stock solution of the impurity (1 mg/mL) in acetonitrile. Prepare a standard mixture containing Azithromycin (2 mg/mL) and the impurity (2 ug/mL). Use a C18 column (4.6 × 150 mm, 5 um) at 40degC. Mobile phase: acetonitrile: 0.1 M ammonium acetate (pH 6.5) (60:40). Flow rate: 1.0 mL/min. Detection: UV at 210 nm or ELSD. The relative retention time (RRT) of the impurity is approximately 0.7 relative to azithromycin. Validate linearity (0.1-10 ug/mL). The reference standard is stored at -20degC. For LC-MS, use positive mode with m/z 577 [M+H]+.
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| Cell Assay |
General protocol for in vitro cell-based experiments: For a forced degradation study, dissolve azithromycin (10 mg) in 1 mL of 0.1 M HCl. Incubate at 60degC for 4 h. Neutralize. Analyze by HPLC. The impurity peak will appear. This demonstrates the degradation profile. No cell culture is required.
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| Animal Protocol |
General protocol for in vivo animal experiments: For a pharmacokinetic study, administer azithromycin (10 mg/kg, PO) to rats. Collect blood at 0, 1, 2, 4, 8, 12, 24, 48, 72 h. Extract plasma with acetonitrile. Analyze by LC-MS/MS. The level of this impurity in plasma is usually <5% of the parent drug. This is a PK study, not an efficacy model.
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| ADME/Pharmacokinetics |
General pharmacokinetic properties: This impurity (MW 576.76) is not a drug. It is a macrolide derivative. It is soluble in organic solvents. For storage, the reference standard should be stored at -20degC, protected from light. The product is for research use only. The compound is a metabolite of Azithromycin. It is an impurity and is used as a reference standard for quality control. This product is strictly intended for laboratory, research, analytical, and scientific use only. It is not meant for human consumption, therapeutic use, or any form of clinical application.
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| Additional Infomation |
Descladinose 6-N-desmethyl azithromycin is also known as Teramycin impurity and CP 60300. It is a key reference standard for the European Pharmacopoeia (EP) and USP for azithromycin. It is a white to off-white solid. The product is for analytical and research purposes only. For research use only.
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| Molecular Formula |
C29H56N2O9
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|---|---|
| Molecular Weight |
576.76
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| Exact Mass |
576.399
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| CAS # |
111247-94-0
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| PubChem CID |
59037908
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| Appearance |
Typically exists as solids at room temperature
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| Hydrogen Bond Donor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
40
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| Complexity |
818
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| Defined Atom Stereocenter Count |
14
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| SMILES |
CC[C@@H]1[C@@]([C@@H]([C@H](NC[C@@H](C[C@@]([C@@H]([C@H]([C@@H]([C@H](C(=O)O1)C)O)C)O[C@H]2[C@@H]([C@H](C[C@H](O2)C)N(C)C)O)(C)O)C)C)O)(C)O
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| InChi Key |
LOMZTTMTKSVHAG-NHUOXGILSA-N
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| InChi Code |
InChI=1S/C29H56N2O9/c1-11-21-29(8,37)24(34)19(6)30-14-15(2)13-28(7,36)25(17(4)22(32)18(5)26(35)39-21)40-27-23(33)20(31(9)10)12-16(3)38-27/h15-25,27,30,32-34,36-37H,11-14H2,1-10H3/t15-,16-,17+,18-,19-,20+,21-,22+,23-,24-,25-,27+,28-,29-/m1/s1
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| Chemical Name |
(2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-11-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-3,4,10,13-tetrahydroxy-3,5,8,10,12,14-hexamethyl-1-oxa-6-azacyclopentadecan-15-one
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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) |
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 | 1.7338 mL | 8.6691 mL | 17.3382 mL | |
| 5 mM | 0.3468 mL | 1.7338 mL | 3.4676 mL | |
| 10 mM | 0.1734 mL | 0.8669 mL | 1.7338 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.
Products are for research use only; We do not sell to patients
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