Ebastine

SKU: orb1223688

Description

Ebastine is a potent H1-histamine receptor antagonist, used for allergic disorders.(In Vitro):Ebastine (10-500 ng/mL; 24-48 hours) treatment significantly increases the proliferation of HFDPC.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.\n(In Vivo):In rats, after intravenous administration of [14C]Ebastine at 2 mg/kg, the plasma level of radioactivity decreased biphasically with α-phase half-life (t1/2 α) of 1.6 h and β-phase half-life (t1/2 β) of 3.1 h.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.

Key Properties

• CAS Number: 90729-43-4
• MW: 469.66
• Purity: >98% (HPLC)
• Formula: C₃₂H₃₉NO₂
• SMILES: O=C(CCCN1CCC(OC(C2=CC=CC=C2)C3=CC=CC=C3)CC1)C4=CC=C(C(C)(C)C)C=C4
• Target: Histamine Receptor
• Solubility: Ethanol: 11 mg/mL (23.42 mM); DMSO: 2 mg/mL (4.25 mM)

Bioactivity

• In Vivo:
  In rats, after intravenous administration of [14C]Ebastine at 2 mg/kg, the plasma level of radioactivity decreased biphasically with α-phase half-life (t1/2 α) of 1.6 h and β-phase half-life (t1/2 β) of 3.1 h. 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.
• In Vitro:
  Ebastine (10-500 ng/mL; 24-48 hours) treatment significantly increases the proliferation of HFDPC. 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. Cell Proliferation Assay Cell line: Human follicle dermal papilla cells (HFDPC). Concentration: 10 ng/mL, 50 ng/mL, 100 ng/mL, 200 ng/mL, 500 ng/mL. Incubation time: 24 hours, 48 hours. Result: The proliferative activity in cells was significantly enhanced. Western blot analysis. Cell line: Human follicle dermal papilla cells (HFDPC). Concentration: 10 ng/mL, 50 ng/mL, 100 ng/mL, 200 ng/mL, 500 ng/mL. Incubation time: 24 hours. Result: The expression levels of cell-cycle regulatory proteins and an antiapoptotic protein were increased in HFDPC.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LAS-W 090 | RP 64305

Quick Database Links

Gene Symbol

Histamine Receptor