Ebastine-d₆  (Synonyms: LAS-W 090-d₆; RP64305-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^[1].

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.

In rats, after intravenous administration of [¹⁴C]Ebastine at 2 mg/kg, the plasma level of radioactivity decreased biphasically with α-phase half-life (t_1/2 α) of 1.6 h and β-phase half-life (t_1/2 β) of 3.1 h^[4].
Following oral administration of [¹⁴C]Ebastine at a dose of 2 mg/kg, the plasma level reached the maximum (C_max) of 102 ng eq./ml at 2 h and decreased monophasically with t_1/2 of 3.9 h. At 20 mg/kg, a monophasic decrease is also observed with C_max of 1110 ng eq./ml at 4 h and with t_1/2 of 4.0 h^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

475.69

C₃₂H₃₃D₆NO₂

90729-43-4

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]

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]