Benztropine mesylate(Synonyms: 甲磺酸苯扎托品; Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate)

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Benztropine mesylate (Synonyms: 甲磺酸苯扎托品; Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate) 纯度: 99.86%

Benztropine mesylate (Benzatropine 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 re-uptake) 抑制剂。Benztropine mesylate 也是一种人 D2 多巴胺受体 (human D2 dopamine receptor) 的变构拮抗剂，并且还具有抗癌症干细胞的作用。

Benztropine mesylate(Synonyms: 甲磺酸苯扎托品; Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate)

Benztropine mesylate Chemical Structure

CAS No. : 132-17-2

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥500 In-stock
500 mg ￥400 In-stock
1 g ￥500 In-stock
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10 g   询价  

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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 a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[1][2].

IC50 & Target[1]

Human D2 Receptor

 

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 IC50 of ~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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50 of ~5 μM.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

403.54

Formula

C22H29NO4S
CAS 号

132-17-2
中文名称

甲磺酸苯扎托品；甲磺酰苯扎托品
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Jihong Cui, et al. New use of an old drug: inhibition of breast cancer stem cells by benztropine mesylate. Oncotarget. 2017 Jan 3;8(1):1007-1022.

    [2]. Santosh S Kulkarni, et al. Comparative structure-activity relationships of benztropine analogues at the dopamine transporter and histamine H(1) receptors. Bioorg Med Chem. 2006 Jun 1;14(11):3625-34.

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