| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Triprolidine-d8 hydrochloride exerts its effects by binding to the histamine H1 receptor in the body. The binding blocks the action of endogenous histamine, preventing it from exerting its effects on tissues and thereby alleviating symptoms associated with allergic responses. The deuterium atoms do not alter the binding affinity or efficacy of the compound, making it an ideal tracer for PK studies.
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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 effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
The labeled compound, (E/Z)-Triprolidine-d8 hydrochloride, is a first-generation antihistamine with anticholinergic properties. It is used to treat and prevent symptoms associated with allergies, including allergic rhinitis, as well as to provide relief for flu-like symptoms. Its utility in research stems from its use as an analytical tracer. |
| ln Vivo |
The unlabeled parent compound Triprolidine is an antihistaminic agent used in vivo to treat allergic conditions. The deuterated analog is not used as a therapeutic agent but is employed in animal models as a tracer to study the absorption, distribution, metabolism, and excretion (ADME) of the parent drug.
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| Enzyme Assay |
There is no standard enzyme/receptor binding protocol for the labeled standard itself. For receptor binding studies, the unlabeled compound is the active agent. The labeled version is used in analytical workflows to measure the concentration of the active compound in receptor binding buffers or tissue homogenates via LC-MS/MS.
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| Cell Assay |
This compound is not used for direct cell-based experiments for its own activity. In a typical cell-based study, cells (e.g., mast cells) are treated with unlabeled Triprolidine to study its effects on histamine release. The deuterated standard is added to the culture medium or cell lysate during LC-MS/MS sample preparation to quantify the amount of drug that has entered the cells.
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| Animal Protocol |
In an in vivo PK study, animals (e.g., Sprague-Dawley rats) are administered unlabeled Triprolidine orally or intravenously. Blood samples are collected at various time points. The plasma is separated, and a known amount of (E/Z)-Triprolidine-d8 hydrochloride is added as an internal standard. The Triprolidine concentration is then measured by LC-MS/MS to determine its PK parameters.
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| ADME/Pharmacokinetics |
As an analytical standard, (E/Z)-Triprolidine-d8 hydrochloride is not administered to determine its own PK profile. For in vivo analysis where it is used as a standard, it is formulated as a solution in an appropriate solvent, such as methanol, acetonitrile, or water, at a specific concentration (e.g., 1 mg/mL) and stored frozen to maintain stability.
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| Toxicity/Toxicokinetics |
General toxicity for the labeled compound is expected to be comparable to the parent drug, Triprolidine, which is a first-generation antihistamine known to cause sedation and anticholinergic side effects (e.g., dry mouth, drowsiness). The labeled compound is intended for research use only at small scale and is not for human therapeutic use.
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| References | |
| Additional Infomation |
(E/Z)-Triprolidine-d8 hydrochloride is a stable isotope-labeled internal standard. The mixture of cis/trans isomers is used to represent the parent drug. The deuterium labeling allows for its use in bioanalytical method development and validation, and it is an essential tool for the quantitative analysis of Triprolidine in Dried Blood Spots (DBS) for regulatory studies.
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| Molecular Formula |
C19H15D8CLN2
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|---|---|
| Molecular Weight |
322.90
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| Exact Mass |
322.205
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| CAS # |
1795134-06-3
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| Related CAS # |
Triprolidine;486-12-4
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| PubChem CID |
126480243
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
336
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C1(C(C(N(C1([2H])[2H])C/C=C(/C2=CC=C(C=C2)C)\C3=CC=CC=N3)([2H])[2H])([2H])[2H])[2H].Cl
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| InChi Key |
WYUYEJNGHIOFOC-GTULIFIYSA-N
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| InChi Code |
InChI=1S/C19H22N2.ClH/c1-16-7-9-17(10-8-16)18(19-6-2-3-12-20-19)11-15-21-13-4-5-14-21;/h2-3,6-12H,4-5,13-15H2,1H3;1H/b18-11-;/i4D2,5D2,13D2,14D2;
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| Chemical Name |
2-[(Z)-1-(4-methylphenyl)-3-(2,2,3,3,4,4,5,5-octadeuteriopyrrolidin-1-yl)prop-1-enyl]pyridine;hydrochloride
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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 | 3.0969 mL | 15.4847 mL | 30.9693 mL | |
| 5 mM | 0.6194 mL | 3.0969 mL | 6.1939 mL | |
| 10 mM | 0.3097 mL | 1.5485 mL | 3.0969 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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