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Purity: ≥98%
Fexofenadine HCl (formerly MDL-16455A; Allegra; Terfenidine carboxylate; Telfast) is a potent histamine H1 receptor antagonist (antihistamine agent) used in the treatment of allergy symptoms such as hay fever, nasal congestion, and urticaria. Fexofenadine belongs to the second generation of antihistamines because, in contrast to first-generation antihistamines, it is less able to sedate people by crossing the blood-brain barrier.Fexofenadine has an IC50 value of 95.5 nM and demonstrates a strong, concentration-dependent anti-anaphylactic effect. For the 5-HT2A receptors from the rat caudal artery with a pA2 of 5.2, fexofenadine only exhibits a weak competitive antagonist behavior. On the P-gp-mediated secretion of Fexofenadine, verapamil's half-life (IC50) is 8.44 mM.
| Targets |
Histamine H1 receptor ( IC50 = 246 nM )
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| ln Vivo |
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| Cell Assay |
Fexofenadine hydrochloride (MDL-16455 hydrochloride) (100 µM; 1 hour) efficiently inhibits phosphorylated p38 activation in histamine-induced nasal fibroblasts.
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| 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 |
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| References |
| Molecular Formula |
C32H40CLNO4
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| Molecular Weight |
538.12
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| Exact Mass |
537.26
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| Elemental Analysis |
C, 71.42; H, 7.49; Cl, 6.59; N, 2.60; O, 11.89
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| CAS # |
153439-40-8
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| Related CAS # |
Fexofenadine; 83799-24-0; Fexofenadine-d6; 548783-71-7; Fexofenadine-d10 hydrochloride; 1215821-44-5
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| Appearance |
Solid powder
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| 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.Cl
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| InChi Key |
RRJFVPUCXDGFJB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H39NO4.ClH/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);1H
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| Chemical Name |
2-[4-[1-hydroxy-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butyl]phenyl]-2-methylpropanoic acid;hydrochloride
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| Synonyms |
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.65 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.65 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8583 mL | 9.2916 mL | 18.5832 mL | |
| 5 mM | 0.3717 mL | 1.8583 mL | 3.7166 mL | |
| 10 mM | 0.1858 mL | 0.9292 mL | 1.8583 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 |
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