Buclizine dihydrochloride 是具有口服活性的抗组胺、抗过敏化合物。Buclizine dihydrochloride 是大鼠的强致畸剂，并具有抗肿瘤活性。
| 生物活性 | Buclizine dihydrochloride is an orally activeantihistamineantiallergic compound. Buclizine dihydrochloride is a potent teratogen in the rat and shows anti-tumor activity[1][2][3]. |
体外研究
(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].
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). |
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. |
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体内研究
(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].
| 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 2.5 mg/mL(4.94 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9765 mL | 9.8824 mL | 19.7648 mL | | 5 mM | --- | --- | --- | | 10 mM | --- | --- | --- |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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