| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Hydroxyzine D8 targets the histamine H1 receptor, a G-protein-coupled receptor that mediates the effects of histamine in allergic and inflammatory responses. By acting as an antagonist at this receptor, it blocks histamine-induced vasodilation, increased vascular permeability, and smooth muscle contraction, thereby alleviating allergy symptoms.
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|---|---|
| ln Vitro |
In vitro, Hydroxyzine D8 acts as a histamine H1-receptor antagonist. Its deuterium labeling does not significantly alter its pharmacological activity compared to the parent compound, but it serves as an internal standard for analytical purposes.
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| ln Vivo |
In vivo, Hydroxyzine D8 is expected to exhibit the same pharmacological effects as Hydroxyzine, including antihistaminic, antiemetic, anxiolytic, and sedative properties. As a deuterated compound, it is primarily used as an internal standard in mass spectrometry-based assays to quantify Hydroxyzine levels in biological samples.
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| Enzyme Assay |
As a deuterated internal standard, Hydroxyzine D8 is not typically used in enzyme or receptor binding assays. However, its parent compound, Hydroxyzine, binds to the histamine H1 receptor. Binding affinity can be assessed using radioligand binding assays with membrane preparations from cells expressing the H1 receptor.
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| Cell Assay |
Hydroxyzine D8 is used as an internal standard in cell-based or biological sample analysis. In a typical protocol, a known amount of Hydroxyzine D8 is added to a sample (e.g., plasma, urine, or cell culture medium) containing Hydroxyzine. The sample is then processed and analyzed by LC-MS/MS to quantify Hydroxyzine levels.
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| Animal Protocol |
In vivo studies with Hydroxyzine D8 involve its use as an internal standard in pharmacokinetic studies. A known amount of the deuterated compound is administered alongside or separately from Hydroxyzine, and blood samples are collected at various time points. The ratio of Hydroxyzine to Hydroxyzine D8 is measured by LC-MS/MS to determine pharmacokinetic parameters.
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| ADME/Pharmacokinetics |
As a deuterated compound, Hydroxyzine D8 is expected to have similar pharmacokinetic properties to Hydroxyzine. It is well absorbed after oral administration and widely distributed throughout the body. It is metabolized in the liver and excreted in the urine.
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| Toxicity/Toxicokinetics |
Hydroxyzine is generally well-tolerated. Common side effects include drowsiness, dry mouth, and dizziness. Rare but serious side effects include QT prolongation and tardive dyskinesia. As an internal standard, Hydroxyzine D8 is used in trace amounts and does not contribute to toxicity.
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| References | |
| Additional Infomation |
Hydroxyzine D8 is a deuterium-labeled version of Hydroxyzine, primarily used as an internal standard for the quantification of Hydroxyzine in biological samples using LC-MS/MS. It is not intended for therapeutic use.
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| Molecular Formula |
C21H19D8N2O2CL
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|---|---|
| Molecular Weight |
382.953574224
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| Exact Mass |
382.226
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| CAS # |
1189480-47-4
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| Related CAS # |
Hydroxyzine;68-88-2
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| PubChem CID |
45039540
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| Appearance |
White to off-white solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
26
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| Complexity |
376
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(O)COCCN1C([2H])([2H])C([2H])([2H])N(C(C2=CC=C(Cl)C=C2)C2=CC=CC=C2)C([2H])([2H])C1([2H])[2H]
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| InChi Key |
ZQDWXGKKHFNSQK-BGKXKQMNSA-N
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| InChi Code |
InChI=1S/C21H27ClN2O2/c22-20-8-6-19(7-9-20)21(18-4-2-1-3-5-18)24-12-10-23(11-13-24)14-16-26-17-15-25/h1-9,21,25H,10-17H2/i10D2,11D2,12D2,13D2
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| Chemical Name |
2-[2-[4-[(4-chlorophenyl)-phenylmethyl]-2,2,3,3,5,5,6,6-octadeuteriopiperazin-1-yl]ethoxy]ethanol
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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 | 2.6113 mL | 13.0565 mL | 26.1131 mL | |
| 5 mM | 0.5223 mL | 2.6113 mL | 5.2226 mL | |
| 10 mM | 0.2611 mL | 1.3057 mL | 2.6113 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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