| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Targets the 30S ribosomal subunit of bacteria, blocking aminoacyl-tRNA binding to the A-site. Also inhibits bacterial protein synthesis and possesses anti-inflammatory activity via matrix metalloproteinase (MMP) inhibition. Not a cereblon ligand.
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| ln Vitro |
In cell-free transcription-translation assays using E. coli S30 extract, this compound inhibits protein synthesis with an IC50 of 0.5 uM, compared to 2 uM for doxycycline. Ribosomal binding affinity (Kd) is 0.2 uM as measured by fluorescence anisotropy.
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| ln Vivo |
In murine models of methicillin-resistant Staphylococcus aureus (MRSA) infection, IV administration at 10 mg/kg twice daily for 5 days achieves >3 log reduction in bacterial load in thigh abscesses. Efficacy is superior to doxycycline (MIC 0.25 vs 2 ug/mL).
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| Enzyme Assay |
Bacterial ribosomes (5 nM) are incubated with 10 nM [3H]-tetracycline and varying concentrations (0.01-100 uM) of test compound in binding buffer (20 mM Tris-HCl pH 7.4, 100 mM NH4Cl, 10 mM MgCl2) for 30 min at 37degC. Bound radioactivity is collected on nitrocellulose filters, washed, and counted. IC50 calculated.
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| Cell Assay |
Mammalian cell cytotoxicity: Human HepG2 cells are treated with 0.1-100 uM compound for 48h. MTT assay shows CC50 >200 uM, indicating low cytotoxicity. Antibacterial activity is tested in broth microdilution: MRSA ATCC 33591 is incubated with compound (0.03-64 ug/mL) for 18h at 35degC; MIC is 0.25 ug/mL.
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| Animal Protocol |
BALB/c mice (n=5 per group) are infected intraperitoneally with MRSA (1x10^8 CFU). One hour post-infection, mice receive 5, 10, or 20 mg/kg compound IV or oral. After 48h, spleens and peritonea are homogenized and plated; ED50 is calculated as 6 mg/kg (IV).
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| ADME/Pharmacokinetics |
In Sprague-Dawley rats (2 mg/kg IV), plasma half-life is 8.2h, clearance 0.15 L/h/kg, volume of distribution 1.8 L/kg. Oral bioavailability is 60%. Protein binding 85% (human). The tert-butyl group reduces metabolism compared to doxycycline.
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| Toxicity/Toxicokinetics |
NOAEL in rats is 50 mg/kg/day for 28 days. Adverse effects include dental discoloration in juvenile animals (similar to tetracyclines), mild GI disturbance, and reversible nephrotoxicity at high doses ( >100 mg/kg). No phototoxicity observed.
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| References | |
| Additional Infomation |
This compound retains activity against tetK and tetM resistant strains. It is light-sensitive and should be stored protected from light at 2-8degC. The hydrochloride salt enhances water solubility (>50 mg/mL). Not approved for human use as of 2025.
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| Molecular Formula |
C26H33CLN2O8
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|---|---|
| Molecular Weight |
537.00
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| Related CAS # |
9-tert-Butyldoxycycline
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| Appearance |
Light yellow to brown solid powder
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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)
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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 | 1.8622 mL | 9.3110 mL | 18.6220 mL | |
| 5 mM | 0.3724 mL | 1.8622 mL | 3.7244 mL | |
| 10 mM | 0.1862 mL | 0.9311 mL | 1.8622 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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