Benztropine mesylate 是一种具有口服活性的中枢性抗胆碱能剂，可用于帕金森氏病的研究。Benztropine mesylate 是一种抗组胺剂和多巴胺再摄取 (dopamine reuptake) 抑制剂。Benztropine mesylate 也是一种人 D2多巴胺受体 (human D2dopamine receptor) 的变构拮抗剂，并且具有抗癌作用。
| 生物活性 | Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and adopamine re-uptakeinhibitor. Benztropine mesylate is also ahuman D2dopamine receptorallosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[1][2]. |
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体外研究
(In Vitro) | Benztropine mesylate (0.1-10 μM; 72 hours) treatment inhibits the cell growth of MDA-MB-231 cells with an IC50of ~5 μM. In MDA-MB-231 cells and 4T1-luc2 cells, Benztropine mesylate reduces the size as well as the number of mammospheres significantly in a dose-dependent manne[1].
Benztropine mesylate inhibits functions of cancer stem cells (CSCs) via the acetylcholine receptors, dopamine transporters/receptors, and/or histamine receptors[1].
Benztropine mesylate induces the differentiation of oligodendrocytes through M1 and M3 muscarinic receptors and enhanced re-myelination[1].
Cell Viability Assay[1] | Cell Line: | MDA-MB-231 cells | | Concentration: | 0.1 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM | | Incubation Time: | 72 hours | | Result: | Inhibited the cell growth of MDA-MB-231 cells with an IC50of ~5 μM. |
Cell Proliferation Assay[1] | Cell Line: | MDA-MB-231 cells | | Concentration: | 0, 1, 2, 5 μM | | Incubation Time: | 4-6 days | | Result: | Suppressed mammosphere formation and self-renewal capacities of BCSCs in a dose-dependent manner in vitro. |
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体内研究
(In Vivo) | Benztropine mesylate (1.5 mg/kg; daily; for 3 weeks; Balb/c mice) treatment significantly reduces both tumor size and tumor weight in a 4T1 mouse model[1].
| Animal Model: | Balb/c mice bearing 4T1 breast tumors | | Dosage: | 1.5 mg/kg | | Administration: | Injection; 3 weeks | | Result: | Reduced the tumor size and weight significantly without body weight changing. |
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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 : 100 mg/mL(247.81 mM;Need ultrasonic) H2O : 100 mg/mL(247.81 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.4781 mL | 12.3903 mL | 24.7807 mL | | 5 mM | 0.4956 mL | 2.4781 mL | 4.9561 mL | | 10 mM | 0.2478 mL | 1.2390 mL | 2.4781 mL |
*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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 100 mg/mL (247.81 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.20 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.20 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.20 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.20 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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