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| 1mg |
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| Other Sizes |
| Targets |
The unlabeled 5-HIAA is the major metabolite of serotonin (5-HT). Serotonin is a key neurotransmitter and hormone that acts on a family of 5-HT receptors (GPCRs and ion channels). 5-HIAA is formed from serotonin via a 5-Hydroxy Indole-3-acetaldehyde intermediate by the action of aldehyde dehydrogenase. It is inactive and is excreted in the urine. As a metabolite, it serves as a biomarker for serotonin production. The d6-labeled standard does not directly interact with enzymes or receptors.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
As an internal standard, 5-Hydroxyindole-3-acetic acid-d6 has no biological activity. The non-labeled 5-HIAA is the major metabolite of serotonin and is used as a biomarker for serotonin turnover. In vitro, levels of 5-HIAA in cell culture media can be measured to assess the activity of the serotonin pathway, particularly in models of neuroendocrine tumors. |
| ln Vivo |
In vivo, the unlabeled 5-HIAA is a major metabolite of serotonin. Its concentration in urine (measured over 24 hours) is a well-established biomarker for the diagnosis and monitoring of carcinoid tumors and other neuroendocrine tumors that produce excess serotonin. Elevated levels indicate increased serotonin production. The deuterated compound serves as an internal standard for this diagnostic test.
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| Enzyme Assay |
The labeled internal standard is not used in enzyme/receptor binding assays. It is used in analytical method development for LC-MS/MS. A standard protocol involves spiking a known amount of the d6-labeled internal standard into biological samples (e.g., urine, plasma, tissue homogenate). After sample preparation (protein precipitation, dilution, or solid-phase extraction), the sample is analyzed by LC-MS/MS. The deuterated standard and the non-labeled analyte are detected in MRM mode, and the peak area ratio is used for precise quantification.
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| Cell Assay |
For in vitro cellular metabolism studies, cultured cells (e.g., neuroendocrine cell lines like BON-1) are treated with compounds that affect serotonin synthesis or release. The culture media is collected, and the d6-labeled internal standard is spiked in. After protein precipitation and centrifugation, the supernatant is analyzed by LC-MS/MS. The concentration of 5-HIAA in the media is used as an indirect measure of serotonin release and metabolism.
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| Animal Protocol |
The internal standard is not administered directly. In animal studies (e.g., mice with xenografted tumors), urine or plasma is collected. The d6-labeled internal standard is spiked into the samples before LC-MS/MS analysis. This allows for the accurate measurement of the endogenous biomarker 5-HIAA, which can be used to monitor tumor burden or the pharmacodynamic effect of drugs targeting serotonin synthesis (e.g., tryptophan hydroxylase inhibitors).
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| ADME/Pharmacokinetics |
5-Hydroxyindole-3-acetic acid-d6 has a molecular formula of C10H3D6NO3 and a molecular weight of 197.22. It is soluble in DMSO, methanol, and ethyl acetate. For LC-MS/MS applications, it is typically dissolved in a suitable solvent such as water or methanol to prepare stock solutions. The deuterated compound is stable and co-elutes with the non-labeled analyte during chromatography. Long-term storage should be at -20degC, protected from light and moisture.
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| Toxicity/Toxicokinetics |
The deuterated compound is non-toxic at the trace concentrations used for analytical purposes. The unlabeled parent, 5-HIAA, is an endogenous metabolite and is non-toxic at physiological levels. The compound is "For research use only" and not for human therapeutic or diagnostic use.
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| References | |
| Additional Infomation |
5-Hydroxyindole-3-acetic acid-d6 is a research-grade stable isotope-labeled chemical used as an internal standard for LC-MS/MS quantification. The unlabeled 5-HIAA is the major metabolite of serotonin and is used as a biomarker for neuroendocrine tumors. This product is for research use only (RUO) and is not a clinical drug; it has no FDA approval for human therapy. It is used in clinical chemistry and pharmacology for the validation of assays measuring serotonin turnover.
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| Molecular Formula |
C10H3D6NO3
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| Molecular Weight |
197.22
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| Related CAS # |
5-Hydroxyindole-3-acetic acid;54-16-0
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| Appearance |
White to off-white 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 |
| 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 | 5.0705 mL | 25.3524 mL | 50.7048 mL | |
| 5 mM | 1.0141 mL | 5.0705 mL | 10.1410 mL | |
| 10 mM | 0.5070 mL | 2.5352 mL | 5.0705 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.