1. Buclizine

Buclizine is an orally active antihistamine antiallergic compound. Buclizine is a potent teratogen in the rat and shows anti-tumor activity.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Buclizine dihydrochloride) usually boasts enhanced water solubility and stability.

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Buclizine Chemical Structure

Buclizine Chemical Structure

CAS No. : 82-95-1

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Description

Buclizine is an orally active antihistamine antiallergic compound. Buclizine 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].

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

Cell Proliferation Assay[2]

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

Cell Cycle Analysis[2]

Cell Line: MCF-7 cells
Concentration: 9.625, 19.25, 38.5, and 77 μM
Incubation Time: 72 hours
Result: Increased the percentages of cells in the G1 phase to 73% at 77 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

Buclizine dihydrochloride (30-200 mg/kg; tenth to fifteenth and twelfth to fifteenth days of gestation) shows potent teratogens in the rat[3].

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

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

433.03

Formula

C28H33ClN2

CAS No.
SMILES

CC(C1=CC=C(CN2CCN(C(C3=CC=C(Cl)C=C3)C4=CC=CC=C4)CC2)C=C1)(C)C

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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Help & FAQs
  • 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
Cat. No.:
HY-A0128
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