| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Tetracycline
Rolitetracycline targets the 30S ribosomal subunit in bacteria. It reversibly binds to this subunit, preventing the binding of tRNA to the mRNA-ribosome complex. This action interferes with protein synthesis, exerting bacteriostatic and bactericidal activities. It also inhibits HIV-1 integrase, blocks Aβ fibril formation, and suppresses dengue virus proliferation. |
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| ln Vitro |
In vitro, Rolitetracycline demonstrates broad-spectrum antibacterial activity against a wide range of Gram-positive and Gram-negative bacteria. It binds to and stabilizes bovine serum albumin. It also inhibits HIV-1 integrase and blocks Aβ fibril formation via a specific three-dimensional pharmacophore conformation. These activities highlight its diverse biological effects beyond antibacterial activity.
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| ln Vivo |
In vivo, Rolitetracycline is used as a broad-spectrum antibiotic for parenteral administration. It is effective in treating various bacterial infections, particularly when high concentrations are needed. It has a role as a protein synthesis inhibitor, an antiprotozoal drug, and a prodrug. However, its use has declined with the development of newer antibiotics.
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| Enzyme Assay |
The in vitro antibacterial activity of Rolitetracycline is assessed using standard susceptibility testing methods, such as broth dilution or disk diffusion assays. These assays measure the minimum inhibitory concentration (MIC) against various bacterial strains. Its ability to bind to the 30S ribosomal subunit can be studied using cell-free translation systems or ribosome binding assays.
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| Cell Assay |
In vitro cellular assays for Rolitetracycline are not typically conducted for its antibacterial effects, as it targets bacteria rather than eukaryotic cells. However, its effects on mammalian cells can be assessed to evaluate potential toxicity or off-target effects. Its ability to inhibit HIV-1 integrase can be studied in cell-based antiviral assays.
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| Animal Protocol |
In vivo animal studies for Rolitetracycline have been conducted in animal models of bacterial infection to establish its efficacy and safety. However, these studies are not extensively detailed in the available literature. Its clinical efficacy has been established in human use for various infections. It is approved for clinical use in some regions.
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| ADME/Pharmacokinetics |
Rolitetracycline is administered parenterally (intravenously or intramuscularly). It is a water-soluble compound that is rapidly distributed in the body. It is excreted primarily by the kidneys. Its pharmacokinetic properties allow for the achievement of high concentrations in the blood and tissues. Detailed parameters are not extensively detailed in the available literature.
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| Toxicity/Toxicokinetics |
Rolitetracycline has a well-established safety profile typical of tetracycline antibiotics. Common adverse effects include gastrointestinal disturbances, photosensitivity, and tooth discoloration. It is contraindicated in pregnant women and children due to effects on bone and tooth development. Its safety has been established through clinical use.
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| References |
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| Additional Infomation |
Lolitetracycline is a tetracycline derivative in which the amide group is replaced by a pyrrolylmethyl group. It has dual action as an antibacterial agent, a protein synthesis inhibitor, an antigenic agent, and a prodrug. It belongs to the tetracycline class of antibiotics and is also a tertiary α-hydroxy ketone.
Pyrrolylmethyltetracycline. Pyrrolylmethyltetracycline. Indications Lolitetracycline is a broad-spectrum antibiotic used in situations requiring high concentrations or where oral administration is inconvenient. Mechanism of Action Lolitetracycline is a semi-synthetic broad-spectrum tetracycline antibiotic, particularly suitable for situations requiring high concentrations or where oral administration is inconvenient. It can be administered via the parenteral route. Lolitetracycline passively diffuses through porin channels on bacterial membranes and reversibly binds to the 30S ribosomal subunit, preventing the binding of tRNA to the mRNA-ribosome complex, thereby interfering with protein synthesis. Rolitetracycline is a semi-synthetic tetracycline antibiotic used primarily for parenteral administration. Its use has declined with the availability of newer antibiotics with better safety profiles. It is a valuable compound for studying the tetracycline class of antibiotics. It is available as a prescription medication in some regions. |
| Molecular Formula |
C27H33N3O8
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|---|---|
| Molecular Weight |
527.56622
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| Exact Mass |
527.227
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| Elemental Analysis |
C, 61.47; H, 6.30; N, 7.96; O, 24.26
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| CAS # |
751-97-3
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| Related CAS # |
751-97-3 (free);7681-32-5 (nitrate anhydrous);
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| PubChem CID |
54682938
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| Appearance |
Solid powder
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| Density |
1.542g/cm3
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| Boiling Point |
824.37ºC at 760 mmHg
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| Melting Point |
163.5°C
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| Flash Point |
452.363ºC
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| Index of Refraction |
1.713
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| LogP |
0.798
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
38
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| Complexity |
1110
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C[C@@]1(O)C2=C(C(C3=C(O)[C@@]4(O)[C@H]([C@H](N(C)C)C(O)=C(C(NCN5CCCC5)=O)C4=O)C[C@@H]31)=O)C(O)=CC=C2
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| InChi Key |
IKQRPFTXKQQLJF-IAHYZSEUSA-N
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| InChi Code |
InChI=1S/C27H33N3O8/c1-26(37)13-7-6-8-16(31)17(13)21(32)18-14(26)11-15-20(29(2)3)22(33)19(24(35)27(15,38)23(18)34)25(36)28-12-30-9-4-5-10-30/h6-8,14-15,20,31-32,35,37-38H,4-5,9-12H2,1-3H3,(H,28,36)/t14-,15-,20-,26+,27-/m0/s1
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| Chemical Name |
(4S,4aS,5aS,6S,12aR)-4-(dimethylamino)-1,6,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-N-(pyrrolidin-1-ylmethyl)-4,4a,5,5a-tetrahydrotetracene-2-carboxamide
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| Synonyms |
Rolitetracycline; Reverin; Rolitetraciclina; Rolitetracyclinum; Solvocillin; Rolitetracycline Monohydrochloride.
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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) |
H2O : ~10 mg/mL (~18.95 mM)
DMSO : < 1 mg/mL Ethanol : < 1 mg/mL |
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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 | 1.8955 mL | 9.4774 mL | 18.9548 mL | |
| 5 mM | 0.3791 mL | 1.8955 mL | 3.7910 mL | |
| 10 mM | 0.1895 mL | 0.9477 mL | 1.8955 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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