Rolitetracycline
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Rolitetracycline is a highly soluble, broad-spectrum antibiotic derived from tetracycline. Rolitetracycline binds to and stabilizes bovine serum albumin, and also inhibits HIV-1 integrase, blocks Aβ fibril formation and suppresses dengue virus proliferation. Rolitetracycline mediates the inhibition of Aβ fibrils via a specific three-dimensional pharmacophore conformation, and exerts bacteriostatic and bactericidal activities. Rolitetracycline acts synergistically with Penicillin G (HY-N7139) or Cephalothin (HY-B1275A) to alter the effects on microbial growth. Rolitetracycline serves as an important tool compound for the study of bacterial infections (urinary tract infections, sepsis), HIV-1 and dengue virus infections, as well as Alzheimer's disease.
For research use only. We do not sell to patients.
- Purity: 95.0%
- CAS No.: 751-97-3
- Formula: C27H33N3O8
- Molecular Weight:527.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Antibiotic Isoforms
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Biological Activity
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Tetracycline |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | CC50 |
45.5 μM
Compound: rolitetracycline
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Cytotoxicity against CEM cells after 5 days by MTT method
Cytotoxicity against CEM cells after 5 days by MTT method
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[PMID: 17376679] |
| CCRF-CEM | EC50 |
>45.5 μM
Compound: rolitetracycline
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Antiviral activity against HIV1 3B in CEM cells assessed as inhibition of viral-induced cytopathicity
Antiviral activity against HIV1 3B in CEM cells assessed as inhibition of viral-induced cytopathicity
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[PMID: 17376679] |
Rolitetracycline (0.09-2.5 μg/mL, overnight; 0.02-3.12 μg/mL, overnight) exhibits additive or synergistic activity (no antagonism) when combined with penicillin G or cephalothin against 20 E. coli and 14 S. aureus nosocomial strains, with a mean MIC of 1.61 μg/mL for E. coli and 0.28 μg/mL for S. aureus[1].
Rolitetracycline (0.45-1000 μg/mL, 24-72 h) is significantly more active against stable staphylococcal L-forms (cell wall-defective) than their corresponding parent S. aureus strains, with MICs ranging from 0.45 to 3.9 μg/mL for L-forms versus 1.9 to 500 μg/mL for parent strains[1].
Rolitetracycline (250 μM; 18 h) inhibits Aβ 1-40 fibril formation by 34% in a cell-free immunoassay following co-incubation with 11.6 μM Aβ 1-40[2].
Rolitetracycline (20 μM; 18 h) reduces the biological activity of Aβ 1-40 (as measured by MTT reduction inhibition) by 10-20% in IMR32 human neuroblastoma cells following pre-incubation with 11.6 μM Aβ 1-40[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:IMR32 human neuroblastoma cells
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Concentration:20 μM
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Incubation Time:18 h (pre-incubation with Aβ1-40); 24 h (cell incubation)
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Result:Inhibited the Aβ-induced reduction of MTT by 10-20%.
Chemical Information
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CAS No. 751-97-3
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Appearance Solid
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Molecular Weight 527.57
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Formula C27H33N3O8
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Color Light yellow to brown
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SMILES
O=C(C(C1=O)=C(O)[C@@H](N(C)C)[C@]2([H])C[C@]3([H])[C@](C)(O)C4=C(C(C3=C(O)[C@@]21O)=O)C(O)=CC=C4)NCN5CCCC5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
H2O : 10 mg/mL (18.95 mM; Need ultrasonic and warming)
DMSO : 10 mg/mL (18.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Daschner FD, et al. Combination of bacteriostatic and bactericidal drugs: lack of significant in vitro antagonism between penicillin, cephalothin, and rolitetracycline. Antimicrob Agents Chemother. 1976;10(5):802-808. [Content Brief]
[2]. Howlett DR, et al. Common structural features determine the effectiveness of carvedilol, daunomycin and rolitetracycline as inhibitors of Alzheimer beta-amyloid fibril formation. Biochem J. 1999;343 Pt 2(Pt 2):419-423. [Content Brief]
[3]. Choudhary S, et al. Unraveling the energetics and mode of the recognition of antibiotics tetracycline and rolitetracycline by bovine serum albumin. Chem Biol Drug Des. 2012;80(5):693-705. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.8955 mL | 9.4774 mL | 18.9548 mL | 47.3871 mL |
| 5 mM | 0.3791 mL | 1.8955 mL | 3.7910 mL | 9.4774 mL | |
| 10 mM | 0.1895 mL | 0.9477 mL | 1.8955 mL | 4.7387 mL | |
| 15 mM | 0.1264 mL | 0.6318 mL | 1.2637 mL | 3.1591 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
- Rolitetracycline
- 751-97-3
- Antibiotic
- Bacterial
- Dengue Virus
- Amyloid-β
- HIV Integrase
- Aβ fibril
- human immunodeficiency virus type I integrase
- Alzheimer's disease
- human immunodeficiency virus type I
- E. coli
- S. aureus
- bacterial infections
- dengue virus
- bovine serum albumin
- IMR32 human neuroblastoma cells
- Inhibitor
- inhibitor
- inhibit