Scopine

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Chemical Structure| 498-45-3 同义名 : 6,7-Epoxytropine
CAS号 : 498-45-3
货号 : A578511
分子式 : C8H13NO2
纯度 : 98%
分子量 : 155.19
MDL号 : MFCD06658282
存储条件:

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(676.57 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

生物活性
描述 Scopine is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and is used in the treatment of acute circulatory shock. Chlorambucil (CHL), an alkylating agent, as the model therapeutic agent, and used scopine as a novel brain-targeting moiety. The tissue distribution study after i.v. injection revealed that the AUC0-t and Cmax of CHLS in the brain were 14.25- and 12.20-fold of CHL, respectively. Specifically, CHLS (Chlorambucil-Scopine) accumulated in bEnd.3 and C6 cells in an energy-dependent manner. In C6 cells, superior anti-glioma activity with a significantly decreased IC50 of 65.42 nM/mL was observed for CHLS compared to CHL (IC50 > 400 nM/mL). Scopine is a potential brain-targeting moiety for enhancing the brain uptake efficiency of CHL (chlorambucil)[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

6.44mL

1.29mL

0.64mL

32.22mL

6.44mL

3.22mL

64.44mL

12.89mL

6.44mL

参考文献

[1]ecija P, Vallejo-Lopez M, et al. Scopine Isolated in the Gas Phase. Chemphyschem. 2016 Oct 5;17(19):3030-3034.

[2]Wang X, Li J, et al. Scopine as a novel brain-targeting moiety enhances the brain uptake of chlorambucil. Bioconjug Chem. 2014 Nov 19;25(11):2046-54.

[3]Wang X, Li J, Xu C, et al. Scopine as a novel brain-targeting moiety enhances the brain uptake of chlorambucil. Bioconjug Chem. 2014;25(11):2046-2054