Ebastine-d6
Ebastine-d6 is deuterated labeled Ebastine (HY-B0674). Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research.
For research use only. We do not sell to patients.
- Formula: C32H33D6NO2
- Molecular Weight:475.69
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Histamine Receptor Isoforms
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Biological Activity
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Ebastine (10-500 ng/mL; 24-48 hours) treatment significantly increases the proliferation of HFDPC[3].
Ebastine (10-500 ng/mL; 24-48 hours) treatment shows dose-dependent increases in Cyclin D1, Cyclin E1, and Cyclin A expression levels. And the expression levels of Cdk4, Cdk2, and Cdc2 are alos increased. Ebastine treatment elevates expression levels of phospho-AKT and phospho-p44/42 extracellular signal-regulated kinase[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Following oral administration of [14C]Ebastine at a dose of 2 mg/kg, the plasma level reached the maximum (Cmax) of 102 ng eq./ml at 2 h and decreased monophasically with t1/2 of 3.9 h. At 20 mg/kg, a monophasic decrease is also observed with Cmax of 1110 ng eq./ml at 4 h and with t1/2 of 4.0 h[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled Cas 90729-43-4
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Molecular Weight 475.69
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Formula C32H33D6NO2
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SMILES
O=C(C1=CC=C(C=C1)C(C)(C)C)CCCN(CC2)CCC2OC(C3=CC=CC=C3)([2H])C4=C([2H])C([2H])=C([2H])C([2H])=C4[2H]
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Synonyms
LAS-W 090-d6; RP64305-d6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
[2]. Fu-Ming Tsai, et al. Extracellular Signal-Regulated Kinase Mediates Ebastine-Induced Human Follicle Dermal Papilla Cell Proliferation. Biomed Res Int. 2019 Feb 11;2019:6360503. [Content Brief]
[3]. J Sastre. Ebastine in allergic rhinitis and chronic idiopathic urticarial. Allergy. 2008 Dec;63 Suppl 89:1-20. [Content Brief]
[4]. Fujii, et al. Absorption, distribution, metabolism and excretion of [14C]ebastine after a single administration in rats. Arzneimittelforschung. 1994 Apr;44(4):527-38. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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