| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
L-Histidine-d5 has no independent pharmacological target as a stable isotope tracer. The unlabeled L-histidine is an essential amino acid that serves as a precursor for histamine via histidine decarboxylase, and is involved in the regulation of essential trace element absorption (zinc, copper, and iron). It also demonstrates hydroxyl radical and singlet oxygen scavenging capabilities, anti-inflammatory and antioxidant activities, and can cross the blood-brain barrier, making it relevant in neurobiology research.
|
|---|---|
| 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 effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
As a stable isotope tracer, L-Histidine-d5 hydrochloride hydrate is not tested for classical in vitro pharmacological activity. In cell culture studies, it is used as an internal standard added to cell lysates for the quantification of endogenous histidine by LC-MS/MS. The deuterated compound can also be used to trace histidine metabolic pathways and role in enzyme activity, histamine production, and buffering properties in physiological processes. The deuterium label does not alter biological activity. |
| ln Vivo |
L-Histidine-d5 hydrochloride hydrate has no independent in vivo pharmacological activity as a therapeutic agent. It is used in animal studies as a stable isotope tracer to study histidine metabolism, histamine production, and protein synthesis. The compound can also be used as an internal standard for quantifying L-histidine in biological samples such as plasma, urine, and tissues by LC-MS/MS. The deuterated version follows the same ADME properties as natural L-histidine.
|
| Enzyme Assay |
For in vitro enzyme assays using L-Histidine-d5 hydrochloride hydrate as a tracer, the compound is dissolved in water or an appropriate buffer to prepare a stock solution (e.g., 1 mg/mL). The tracer is then added to enzyme assay mixtures (e.g., histidine decarboxylase, histidine ammonia-lyase) at a fixed concentration. Following incubation at 37degC for 0-60 minutes, the reaction is stopped by adding organic solvent. Histamine-d5 or other products are analyzed by LC-MS/MS. The stable isotope label enables quantification without interfering with enzymatic activity.
|
| Cell Assay |
For cell-based studies, cells (e.g., neuronal cell lines, mast cells, or hepatocytes) are cultured in standard medium (DMEM or RPMI-1640 with 10% FBS). After experimental treatments affecting histidine metabolism (e.g., with histamine receptor antagonists or enzyme inhibitors), cell lysates or culture supernatants are collected. L-Histidine-d5 hydrochloride hydrate is added to samples as an internal standard at a fixed concentration (e.g., 10-100 ng/mL). Following protein precipitation with methanol or acetonitrile and centrifugation, samples are analyzed by LC-MS/MS to quantify endogenous L-histidine and histamine levels.
|
| Animal Protocol |
For in vivo studies, L-Histidine-d5 hydrochloride hydrate is not typically administered to animals as a treatment. It is used as an internal standard for quantifying L-histidine in biological samples obtained from animals treated with experimental compounds or subjected to dietary interventions. After collection of plasma, urine, or tissue homogenates, the deuterated internal standard is added at a fixed concentration (e.g., 10-500 ng/mL). Following protein precipitation with methanol or acetonitrile and centrifugation, samples are analyzed by LC-MS/MS to determine absolute L-histidine concentrations.
|
| ADME/Pharmacokinetics |
L-Histidine-d5 hydrochloride hydrate is an internal standard and does not have independent pharmacokinetic parameters. L-Histidine is an essential amino acid with an absorption half-life of approximately 30-60 minutes in humans. It is absorbed from the small intestine via amino acid transporters, distributed to all tissues, and crosses the blood-brain barrier via the large neutral amino acid transporter. Histidine is decarboxylated to histamine primarily in mast cells and neurons. The deuterated version follows identical ADME properties and is used to calibrate analytical methods.
|
| Toxicity/Toxicokinetics |
L-Histidine is a naturally occurring essential amino acid with low toxicity. The LD50 in rodents is >5,000 mg/kg. The deuterated version is chemically identical except for isotopic substitution and exhibits the same safety profile. L-Histidine-d5 hydrochloride hydrate is known to have hydroxyl radical and singlet oxygen scavenging abilities and can cross the blood-brain barrier. Standard laboratory safety precautions apply. Not intended for human consumption.
|
| References | |
| Additional Infomation |
L-Histidine-d5 hydrochloride hydrate is not a drug but a deuterium-labeled stable isotope research reagent. It has no approved therapeutic status, no clinical trial history as a therapeutic agent, and is not intended for human consumption. This compound is used for research applications including NMR spectroscopy to study molecular structures and dynamics, as a tracer in metabolic studies to understand histidine metabolic pathways and histamine production, and as an internal standard for LC-MS quantification of L-histidine in biological samples. Available with ≥95% purity and ≥98 atom% D.
|
| Molecular Formula |
C6H7D5CLN3O3
|
|---|---|
| Molecular Weight |
209.63
|
| Exact Mass |
214.088
|
| CAS # |
2483831-75-8
|
| Related CAS # |
L-Histidine hydrochloride hydrate;5934-29-2
|
| PubChem CID |
162642347
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
13
|
| Complexity |
151
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C([2H])([2H])(C1NC([2H])=NC=1[2H])[C@]([2H])(N)C(=O)O.Cl.O
|
| InChi Key |
CMXXUDSWGMGYLZ-QGRMNJNTSA-N
|
| InChi Code |
InChI=1S/C6H9N3O2.ClH.H2O/c7-5(6(10)11)1-4-2-8-3-9-4;;/h2-3,5H,1,7H2,(H,8,9)(H,10,11);1H;1H2/t5-;;/m0../s1/i1D2,2D,3D,5D;;
|
| Chemical Name |
(2S)-2-amino-2,3,3-trideuterio-3-(2,4-dideuterio-1H-imidazol-5-yl)propanoic acid;hydrate;hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O: 125 mg/mL (582.32 mM)
|
|---|---|
| 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 | 4.7703 mL | 23.8515 mL | 47.7031 mL | |
| 5 mM | 0.9541 mL | 4.7703 mL | 9.5406 mL | |
| 10 mM | 0.4770 mL | 2.3852 mL | 4.7703 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
