| Size | Price | Stock | Qty |
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| 1mg |
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| 2mg | |||
| 5mg | |||
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| Targets |
Fexofenadine D6 targets the histamine H1 receptor. As a deuterated form of fexofenadine, it selectively blocks the H1 receptor, preventing the release of histamine and other inflammatory mediators. The compound is a non-sedating antihistamine. It is used for the treatment of allergy symptoms such as hay fever, nasal congestion, and urticaria. The deuterated form is used as an internal standard for analytical method development.
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| ln Vitro |
In vitro, Fexofenadine D6 is a histamine H1 receptor antagonist. As a deuterated form of fexofenadine, it selectively blocks the H1 receptor. The compound is used as an internal standard for analytical method development and validation. Its receptor binding affinity has been characterized in various in vitro assays. Fexofenadine D6 is a non-sedating antihistamine.
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| ln Vivo |
In vivo, Fexofenadine D6 is used for the treatment of allergy symptoms such as hay fever, nasal congestion, and urticaria. It is a non-sedating drug that selectively blocks the H1 receptor, preventing the release of histamine and other inflammatory mediators. The compound is a second-generation antihistamine. Fexofenadine D6 can be used for quality control applications during commercial production of Fexofenadine.
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| Enzyme Assay |
In vitro receptor binding assays for Fexofenadine D6 involve measuring affinity for the histamine H1 receptor. Radioligand binding displacement studies are performed using membranes from cells expressing the H1 receptor. The compound's binding affinity (Ki) is determined through competitive binding assays. Functional antagonism is assessed by measuring inhibition of histamine-induced signaling such as calcium mobilization. Assays are performed in appropriate buffer systems with positive controls such as known H1 antagonists (e.g., fexofenadine).
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| Cell Assay |
In vitro cell-based assays for Fexofenadine D6 are conducted in cells expressing the histamine H1 receptor. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations. Receptor antagonism is assessed by measuring inhibition of histamine-induced calcium mobilization or other signaling. Cell viability is assessed by standard assays. Experiments are performed in triplicate with appropriate positive (e.g., fexofenadine) and negative (vehicle) controls.
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| Animal Protocol |
Fexofenadine D6 in vivo studies are conducted in animal models of allergic rhinitis and urticaria. Animals are treated with the compound via oral administration. Allergic symptoms such as sneezing, nasal rubbing, and skin reactions are assessed. Histamine-induced responses are measured. For pharmacokinetic studies, blood samples are collected for LC-MS/MS analysis. Animals are monitored for clinical signs. Tissues and blood samples are collected for histopathological and biochemical analysis at study endpoints. Studies are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Fexofenadine D6 (MW 507.69 g/mol, C32H33D6NO4) is the hexa-deuterated form of Fexofenadine. It is a histamine H1 receptor antagonist. The compound is soluble in DMSO and other organic solvents. It is stable under recommended storage conditions. Fexofenadine D6 is used as an internal standard for analytical method development and quality control applications. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution have been characterized for fexofenadine.
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| Toxicity/Toxicokinetics |
Fexofenadine D6 is generally well-tolerated at therapeutic doses. The compound is a second-generation antihistamine with established safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation is available from clinical use data.
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| Additional Infomation |
Fexofenadine D6 is the hexa-deuterated form of Fexofenadine (Allegra, Telfast), a second-generation antihistamine and H1 receptor antagonist. It is used to treat allergic rhinitis and urticaria. The deuterated form is used as an internal standard for analytical method development and quality control. Its molecular formula is C32H33D6NO4 with a molecular weight of 507.69 g/mol. All applications are limited to non-human research use.
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| Molecular Formula |
C₃₂H₃₃D₆NO₄
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|---|---|
| Molecular Weight |
507.69
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| Exact Mass |
507.326
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| CAS # |
548783-71-7
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| Related CAS # |
Fexofenadine; 83799-24-0; Fexofenadine hydrochloride; 153439-40-8; Fexofenadine-d6 Methyl Ester; 1286458-00-1; Fexofenadine-d3; Fexofenadine-d10; 1215900-18-7
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| PubChem CID |
45039254
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| Appearance |
White to off-white solid powder
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| Density |
1.186g/cm3
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| Boiling Point |
697.261ºC at 760 mmHg
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| Melting Point |
193-196ºC
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| Flash Point |
375.49ºC
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| Index of Refraction |
1.597
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| LogP |
5.448
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
37
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| Complexity |
678
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C([2H])([2H])C(C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O)(C(=O)O)C([2H])([2H])[2H]
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| InChi Key |
RWTNPBWLLIMQHL-WFGJKAKNSA-N
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| InChi Code |
InChI=1S/C32H39NO4/c1-31(2,30(35)36)25-17-15-24(16-18-25)29(34)14-9-21-33-22-19-28(20-23-33)32(37,26-10-5-3-6-11-26)27-12-7-4-8-13-27/h3-8,10-13,15-18,28-29,34,37H,9,14,19-23H2,1-2H3,(H,35,36)/i1D3,2D3
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| Chemical Name |
3,3,3-trideuterio-2-[4-[1-hydroxy-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butyl]phenyl]-2-(trideuteriomethyl)propanoic acid
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| Synonyms |
MDL-16455 D6; MDL16455 D6; Fexofenadine-d6; Terfenadine carboxylate-d6
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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 | 1.9697 mL | 9.8485 mL | 19.6971 mL | |
| 5 mM | 0.3939 mL | 1.9697 mL | 3.9394 mL | |
| 10 mM | 0.1970 mL | 0.9849 mL | 1.9697 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02391688 | Completed | Drug: Bupropion Drug: Fexofenadine |
Drug Interaction | Jules Desmeules | November 2014 | Phase 1 |
Products are for research use only; We do not sell to patients
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