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| 1mg |
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| 10mg |
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| Targets |
L-Histidine serves as an inhibitor of mitochondrial glutamine transport and functions as a precursor to histamine via decarboxylation, playing roles in immune regulation and metabolic pathways.
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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].
L-Histidine hydrochloride hydrate demonstrates the ability to scavenge hydroxyl radicals and singlet oxygen, exhibiting antioxidant activities. It also plays a regulatory role in the absorption of trace metals including zinc, copper, and iron, while showing anti-inflammatory properties. |
| ln Vivo |
As an endogenous metabolite, L-histidine participates in diverse physiological processes including protein synthesis, histamine production, and metal ion chelation. Its deuterated or 15N-labeled form is used as a tracer to study metabolic flux and amino acid utilization in vivo.
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| Enzyme Assay |
Non-cell binding assays for labeled amino acids typically utilize no-wash homogeneous binding technologies. Recombinant proteins or purified enzymes are incubated with 15N-labeled L-histidine and other reaction components in assay buffer. After incubation, samples are directly analyzed by mass spectrometry to detect 15N incorporation into target proteins or metabolites. Surface plasmon resonance (SPR) can also be used to measure real-time binding kinetics between 15N-labeled amino acids and specific binding proteins or enzymes, with sensor chips coated with the target protein and analyte flowed across.
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| Cell Assay |
For cellular studies, cells are cultured in media containing L-Histidine-15N at concentrations ranging from 50 to 500 uM for 24-72 hours to allow incorporation into newly synthesized proteins. After incubation, cells are harvested, lysed, and proteins are extracted. Following trypsin digestion, the resulting peptides are analyzed by liquid chromatography-tandem mass spectrometry (LC-MS/MS) to quantify 15N incorporation into specific histidine residues. For metabolic studies, cells are cultured with 15N-labeled histidine for varying time points to track nitrogen flux through histidine metabolic pathways including histamine production.
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| Animal Protocol |
In vivo animal studies typically involve administration of 15N-labeled L-histidine to rodents via intraperitoneal injection or oral gavage at doses ranging from 10 to 100 mg/kg. Blood samples are collected at multiple time points post-administration (0, 1, 2, 4, 8, 12, 24 hours). Various tissues including liver, kidney, muscle, and brain are harvested, and the 15N enrichment in amino acids and proteins is quantified using isotope ratio mass spectrometry (IRMS) or LC-MS/MS. Studies have examined the biodistribution of labeled histidine and its incorporation into tissue proteins to understand whole-body amino acid metabolism.
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| ADME/Pharmacokinetics |
As a stable isotope-labeled endogenous compound, L-Histidine-15N is not typically evaluated for drug-like pharmacokinetic properties. However, L-histidine hydrochloride hydrate has a reported elimination half-life of approximately 0.5-1.5 hours in humans. The compound is rapidly absorbed from the gastrointestinal tract and distributed throughout body tissues. Plasma protein binding is minimal (<10%). Histidine is metabolized through multiple pathways including conversion to histamine via histidine decarboxylase, transamination, and incorporation into proteins. Histidine is also known to be an inhibitor of mitochondrial glutamine transport. Unmetabolized histidine is excreted in urine.
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| Toxicity/Toxicokinetics |
As an endogenous amino acid, L-histidine is generally recognized as safe with low toxicity. The reported oral LD50 in rats for L-histidine is greater than 15,000 mg/kg. The hydrochloride salt form has been used in nutritional supplements and pharmaceutical preparations without significant adverse effects at physiological doses. High doses of histidine may cause headache, nausea, or allergic-type reactions in sensitive individuals due to histamine production. The 15N-labeled form is considered non-toxic for research purposes when handled properly.
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| References |
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
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| Additional Infomation |
L-Histidine-15N is primarily used as a metabolic tracer in drug development and biomedical research for quantitation during the drug development process. It is employed in protein structure and function studies using NMR spectroscopy, in metabolic flux analysis to trace nitrogen metabolism, and as an internal standard for mass spectrometry quantification of histidine in biological samples. The compound serves as a tool for studying amino acid metabolism, protein turnover, and histidine-related disorders including histidinemia.
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| Molecular Formula |
C6H12CLN215NO3
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| Related CAS # |
L-Histidine hydrochloride hydrate;5934-29-2
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 :~125 mg/mL (~593.49 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.) |
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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