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。

价格： ￥500

品牌：medchemexpress(MCE)

货号：HY-B0520A

产品详情

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

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 D₂ dopamine receptor) 的变构拮抗剂，并且具有抗癌作用。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物，拥有着多年的发展历程和丰富的行业经验。从产品的HNMR数据解析到生物活性数据，从客户的询价到产品的售后服务，我们拥有着完善的管理体系，从而保证我们的服务更加高效、准确。努力为中国的医药行业发展注入新的活力，我们将成为您研发工作值得信赖的伙伴。

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].

MCE 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].

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

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00000793	National Institute of Allergy and Infectious Diseases (NIAID)\|Boehringer Ingelheim	HIV Infections\|Peripheral Nervous System Disease		Phase 2
NCT00802100	National Institute of Mental Health (NIMH)	Schizophrenia	December 2008	Phase 4
NCT00000333	National Institute on Drug Abuse (NIDA)\|Washington D.C. Veterans Affairs Medical Center		May 2001	Phase 2

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
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

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. [Content Brief] [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. [Content Brief]