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| Other Sizes |
| Targets |
8-Bromoguanosine targets enzymes involved in nucleoside metabolism, such as nucleoside kinases and nucleoside transporters. As a guanosine analog, it can be phosphorylated by kinases to form nucleotides that may be incorporated into nucleic acids. The bromine substitution at the 8 position can affect base pairing and stacking interactions, making it useful for studying nucleic acid structure and dynamics. The compound may also interact with guanine-binding proteins and receptors. Its use as a biochemical probe allows for the study of nucleoside metabolism and nucleic acid interactions.
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| ln Vitro |
8-Bromoguanosine (16–18 hours) causes YAC cells to become cytotoxic[2]. 8-Bromoguanosine (18 h) stimulates P815 cells' macrophage cytolytic activity[2].
In vitro studies have demonstrated that 8-Bromoguanosine is used as a biochemical probe for studying nucleic acid structure and function. The compound's bromine substitution allows for specific detection and analysis of nucleic acid interactions. It can be phosphorylated by nucleoside kinases to form nucleotides. The compound's effects on enzyme activity have been characterized in various in vitro systems. Its use as a substrate for studying nucleoside metabolism has been documented. These in vitro findings support its applications in nucleic acid research and enzymology. |
| ln Vivo |
In vivo studies of 8-Bromoguanosine are limited, as the compound is primarily used as a research tool for in vitro biochemical studies. As a nucleoside analog, it would be metabolized through standard nucleoside pathways if administered in vivo. The compound's bromine substitution may affect its metabolism and distribution. Its use as a biochemical probe suggests it may be used in cellular or animal studies to trace nucleic acid metabolism. However, comprehensive in vivo studies specifically targeting 8-Bromoguanosine are not well documented in the available literature.
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| Enzyme Assay |
In vitro enzyme assays for 8-Bromoguanosine typically involve testing its activity as a substrate for nucleoside kinases. Enzyme activity is measured by monitoring the phosphorylation of the compound using radiometric or chromatographic methods. The compound's ability to inhibit enzyme activity is assessed by measuring substrate conversion in the presence of varying concentrations of the compound. For nucleic acid studies, the compound's incorporation into RNA or DNA is assessed using biochemical methods. All assays are performed with appropriate controls and standardized protocols to ensure reproducibility of results.
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| Cell Assay |
In vitro cell-based assays for 8-Bromoguanosine involve culturing cells to evaluate its effects on nucleoside metabolism and nucleic acid synthesis. Cells are treated with varying concentrations of the compound and incorporation into nucleic acids is measured using radiolabeling or other detection methods. Cell viability is assessed using MTT or similar colorimetric assays. The compound's effects on cellular metabolism and gene expression are evaluated. All experiments are performed in triplicate with appropriate controls to ensure statistical reliability.
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| Animal Protocol |
In vivo animal experiments for 8-Bromoguanosine would be conducted to evaluate its metabolism and distribution. Animals would be administered the compound and blood and tissue samples collected at various time points. The compound and its metabolites would be measured using appropriate analytical methods. Parameters assessed would include body weight, organ weights, and general health. Control groups receiving vehicle alone would be included for comparison. All procedures would comply with institutional animal care and use committee guidelines. Comprehensive in vivo studies are not well documented in the available literature.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of 8-Bromoguanosine reflect its nature as a nucleoside analog. It has a molecular weight consistent with its formula C10H12BrN5O5. As a nucleoside, it would be transported into cells via nucleoside transporters and metabolized by nucleoside kinases and phosphatases. The compound's bromine substitution may affect its metabolism and stability. Complete pharmacokinetic profiling including half-life, clearance, volume of distribution, and bioavailability would require further systematic studies using appropriate analytical methods such as high-performance liquid chromatography-mass spectrometry.
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| Toxicity/Toxicokinetics |
The toxicity profile of 8-Bromoguanosine has been evaluated in the context of its use as a research chemical. As a nucleoside analog, it may have effects on cellular metabolism and nucleic acid synthesis. Proper handling procedures including use of personal protective equipment are recommended when working with pure compound. The compound is not approved for human therapeutic use and is intended for research purposes only. Long-term toxicity studies would be needed to fully establish its safety profile. The compound's effects on nucleic acid metabolism should be carefully evaluated in safety studies.
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| References |
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| Additional Infomation |
8-Bromoguanosine is a purine nucleoside.
8-Bromoguanosine (CAS# 4016-63-1) is a brominated nucleoside analog of guanosine with the molecular formula C10H12BrN5O5. It is a purine nucleoside where a bromine atom is substituted at the 8 position of the guanine base. The compound is used in biochemical research to study nucleic acid structure and function, as well as enzyme interactions. Brominated nucleosides are often used as probes for studying RNA and DNA interactions, and as substrates for nucleoside kinases. 8-Bromoguanosine is intended for research use only and is not for human therapeutic use. |
| Molecular Formula |
C10H12BRN5O5
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|---|---|
| Molecular Weight |
362.14
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| Exact Mass |
361.002
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| CAS # |
4016-63-1
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| PubChem CID |
135465599
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| Appearance |
White to off-white solid powder
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| Density |
2.6±0.1 g/cm3
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| Boiling Point |
774ºC at 760mmHg
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| Melting Point |
222°C
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| Flash Point |
421.9ºC
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| Vapour Pressure |
1.73E-17mmHg at 25°C
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| Index of Refraction |
1.986
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| LogP |
-0.08
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
479
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C([C@@H]1[C@H]([C@H]([C@@H](O1)N2C3=C(C(=O)NC(=N3)N)N=C2Br)O)O)O
|
| InChi Key |
ASUCSHXLTWZYBA-UMMCILCDSA-N
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| InChi Code |
InChI=1S/C10H12BrN5O5/c11-9-13-3-6(14-10(12)15-7(3)20)16(9)8-5(19)4(18)2(1-17)21-8/h2,4-5,8,17-19H,1H2,(H3,12,14,15,20)/t2-,4-,5-,8-/m1/s1
|
| Chemical Name |
2-amino-8-bromo-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1H-purin-6-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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 | 2.7614 mL | 13.8068 mL | 27.6136 mL | |
| 5 mM | 0.5523 mL | 2.7614 mL | 5.5227 mL | |
| 10 mM | 0.2761 mL | 1.3807 mL | 2.7614 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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