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| 5mg |
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| Targets |
Inosine itself does not bind to a specific receptor to exert pharmacological activity; rather, it serves as a metabolic intermediate in purine salvage and de novo synthesis pathways. The stable isotope-labeled version (Inosine-13C5) is used as a tracer to quantify metabolic flux and study purine metabolism rather than as a direct ligand.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an impact on a drug's pharmacokinetics and metabolic profile, it has drawn attention [1].
Inosine-13C5 does not possess intrinsic biological activity distinct from unlabeled inosine, as its primary utility lies in analytical applications. However, as a tracer, it can be used to quantify endogenous inosine levels and track metabolic transformations in vitro without perturbing biological systems. Its incorporation into drug molecules serves as a quantitative tracer during drug development. |
| ln Vivo |
In vivo, Inosine-13C5 is administered as a metabolic tracer to study purine metabolism and nucleotide turnover. Its heavy isotope label enables precise quantitation of inosine and its metabolites in biological fluids and tissues using LC-MS/MS. The compound is not intended for therapeutic use but rather for pharmacokinetic and metabolic studies.
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| Enzyme Assay |
In enzyme/receptor binding assays, Inosine-13C5 is not directly used as a ligand. Instead, it serves as an internal standard for mass spectrometry-based quantification of unlabeled inosine. The compound is spiked into samples at known concentrations to correct for matrix effects, ionization efficiency, and extraction recovery during LC-MS/MS analysis.
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| Cell Assay |
For cell culture experiments, Inosine-13C5 is added to the medium at defined concentrations (typically 0.1-10 microM) and incubated with cells for specified time points (e.g., 0-48 hours). Cells are harvested, and intracellular metabolites are extracted. The labeled inosine and its labeled metabolites are quantified by LC-MS/MS to trace flux through the purine metabolic pathway.
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| Animal Protocol |
In animal studies, Inosine-13C5 is administered via intravenous, intraperitoneal, or oral routes at doses determined by the experimental design. Blood samples are collected at multiple time points post-administration, and tissues are harvested at the end of the experiment. LC-MS/MS analysis quantifies the labeled compound and its metabolites to assess distribution, metabolism, and excretion.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Inosine-13C5 are similar to those of unlabeled inosine. After administration, inosine is rapidly distributed and metabolized primarily via purine nucleoside phosphorylase (PNP) to hypoxanthine. The half-life is short (minutes in rodents). The 13C label does not alter the metabolic fate, allowing accurate tracking of the compound's disposition.
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| Toxicity/Toxicokinetics |
Inosine-13C5 exhibits the same low toxicity profile as natural inosine, which is generally recognized as safe. No additional toxicity is introduced by the 13C isotope labeling. High doses may cause mild uric acid elevation due to purine metabolism. Comprehensive toxicological evaluation is required only if the compound is intended for therapeutic use, which is not the case.
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| References |
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-239.
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| Additional Infomation |
Inosine-13C5 is a research-grade stable isotope-labeled compound used exclusively for non-clinical studies. It is not intended for human therapeutic use and has not been approved for clinical applications. The 13C labeling enables precise quantitation in LC-MS/MS and NMR studies. This product is supplied as a lyophilized powder with high isotopic purity (≥98%).
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| Molecular Formula |
C513C5H9N4O5
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| Molecular Weight |
270.17
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| Related CAS # |
Inosine;58-63-9;Inosine-2,8-d2;697807-01-5;Inosine-13C
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| Appearance |
Typically exists as solid at room temperature
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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) |
DMSO :~10 mg/mL (~37.01 mM)
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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 | 3.7014 mL | 18.5069 mL | 37.0137 mL | |
| 5 mM | 0.7403 mL | 3.7014 mL | 7.4027 mL | |
| 10 mM | 0.3701 mL | 1.8507 mL | 3.7014 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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