Size | Price | Stock | Qty |
---|---|---|---|
1g |
|
||
2g |
|
||
5g |
|
||
10g |
|
||
Other Sizes |
|
Fexofenadine (MDL-16455A; MDL16455A; Allegra; Terfenidine carboxylate; Telfast) is a histamine H1 receptor antagonist (antihistamine agent) approved for the treatment of allergy symptoms such as hay fever, nasal congestion, and urticaria.
Targets |
H1 Receptor
|
---|---|
ln Vitro |
Fexofenadine (1-100 µM; 1 h) dose-dependently inhibits the expression of IL-6 protein in nasal fibroblasts[2].
Fexofenadine (1-100 µM; 1 h) inhibits the activation of phosphorylated p38 in nasal fibroblasts induced by histamine, but has no effect on pERK or pJNK[2]. |
ln Vivo |
Fexofenadine hydrochloride (oral administration; 5–20 mg/kg; once daily; 3 w) suppresses both eosinophilia and systemic anaphylaxis in C57BL/6 mice infected with T. spiralis.
|
Cell Assay |
Cell Line: Nasal fibroblasts
Concentration: 100 μM Incubation Time: 1 hour Result: Blocked pp38 activation in histamine-induced nasal fibroblasts, showed histamine-induced IL-6 production mediated by the p38 pathway. |
Animal Protocol |
C57BL/6 mice infected with Trichinella spiralis
5, 10 and 20 mg/kg Oral administration; 5, 10 and 20 mg/kg; once daily; 3 weeks |
References |
|
Molecular Formula |
C32H39NO4
|
---|---|
Molecular Weight |
501.65636
|
Exact Mass |
501.29
|
Elemental Analysis |
C, 76.61; H, 7.84; N, 2.79; O, 12.76
|
CAS # |
83799-24-0
|
Related CAS # |
Fexofenadine hydrochloride; 153439-40-8; Fexofenadine-d6; 548783-71-7; Fexofenadine-d6 Methyl Ester; 1286458-00-1; Fexofenadine-d3; Fexofenadine-d10; 1215900-18-7
|
Appearance |
Solid powder
|
SMILES |
CC(C)(C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O)C(=O)O
|
InChi Key |
RWTNPBWLLIMQHL-UHFFFAOYSA-N
|
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)
|
Chemical Name |
2-[4-[1-hydroxy-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butyl]phenyl]-2-methylpropanoic acid
|
Synonyms |
Telfast; Fexofenadine; Allegra; Carboxyterfenadine; MDL 16.455
|
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 |
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) |
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
|
---|---|
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 | 1.9934 mL | 9.9669 mL | 19.9338 mL | |
5 mM | 0.3987 mL | 1.9934 mL | 3.9868 mL | |
10 mM | 0.1993 mL | 0.9967 mL | 1.9934 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 |
NCT05720455 | Not yet recruiting | Drug: Fexofenadine HCL and pseudoephedrine HCL |
Rhinitis Allergic | Sanofi | July 21, 2024 | Phase 4 |
NCT04534153 | Recruiting | Drug: Fexofenadine Hydrochloride without sodium lauryl sulfate Drug: Fexofenadine Hydrochloride with sodium lauryl sulfate |
The Impact of Excipients on Drug Absorption |
University of California, San Francisco |
January 31, 2023 | Early Phase 1 |
NCT05264025 | Recruiting | Drug: Fexofenadine Drug: Placebo |
Rheumatoid Arthritis | October 6 University | October 2002 | Phase 1 Phase 2 |
NCT04726345 | Recruiting | Drug: Fexofenadine Hcl 180Mg Tab Drug: Placebo |
Nephrolithiasis | Columbia University | June 29, 2021 | Phase 2 |
NCT04688788 | Recruiting | Drug: Rituximab Drug: Ocrelizumab Drug: Fexofenadine |
Relapsing Remitting Multiple Sclerosis Primary Progressive Multiple Sclerosis |
Rigshospitalet, Denmark | April 28, 2021 | Phase 3 |
A dose-response analysis of H1R antagonist fexofenadine on IL-6 production was determined by ELISA. Allergy Asthma Immunol Res . 2014 Nov;6(6):567-72. td> |
The effect of H1R antagonist fexofenadine on the phosphorylation of mitogen-activated protein kinases (ERK, p38, JNK) was evaluated by Western blotting (representative of independent experiments). Allergy Asthma Immunol Res . 2014 Nov;6(6):567-72. td> |