Buclizine dihydrochloride is an orally active antihistamine antiallergic compound.

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Buclizine dihydrochloride Chemical Structure

Chemical Structure

CAS No. : 129-74-8

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Description

Buclizine dihydrochloride is an orally active antihistamine antiallergic compound. Buclizine dihydrochloride is a potent teratogen in the rat and shows anti-tumor activity[1][2][3]. In Vitro: Buclizine (0.1-100 μM; 72 h) inhibits growth of MCF-7 cells[2].
Buclizine (9.625-77 μM; 72 h) arrests the cell cycle in the G1 phase in a dose-dependent manner[2].
Buclizine (0-75 μM; 72 h) decreases TCTP (translationally controlled tumor protein) and cell cycle regulatory proteins expression in MCF-7 cells, increases pro-apoptotic MCL-1S expression[2]. In Vivo: Buclizine dihydrochloride (30-200 mg/kg; tenth to fifteenth and twelfth to fifteenth days of gestation) shows potent teratogens in the rat[3].

In Vitro

Cell Proliferation Assay[2].

Cell Line: MCF-7 cells[3].
Concentration: 0-100 μM.
Incubation Time: 72 hours
Result: Showed considerable growth inhibition (IC50=19.18 μM).

Western Blot Analysis[2].

Cell Line: MCF-7 cells
Concentration: 0-75 μM
Incubation Time: 72 hours
Result: Decreased TCTP expression by 40% at 75 μM.
Decreased cyclin D1, cyclin D3, CDK2 and CDK4 expression after 72 h.
In Vivo
Animal Model: Eighty-seven mature female rats weighing 240±20 grams[3].
Dosage: 30, 40, 60, 100, and 200 mg/kg
Administration: 30-200 mg/kg; tenth to fifteenth and twelfth to fifteenth days of gestation
Result: Resulted in malformations in 100% of the young at a dose level of 60-100 mg/kg.
Molecular Weight

505.95

Formula

C28H35Cl3N2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C1=CC=C(CN2CCN(C(C3=CC=C(Cl)C=C3)C4=CC=CC=C4)CC2)C=C1)(C)C.[H]Cl.[H]Cl

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Buclizine dihydrochloride
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HY-A0128A
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