生物活性

Dynasore is a potent GTPases inhibitor and functions on the sites of dynamin1, dynamin2 or Drp1. When tested with HL-1 cells, treated cells with dynasore blocked the endocytic process via inhibiting the activity of dynamin. Using genetically encoded pH-sensitive fluorescent probe synaptopHluorin to study the role of dynasore in the synapses expressing spH, and the results showed that dyansore treatment resulted in the normal stimulus-triggered increase in fluorescence intensity via reducing the GTPase activity of dynamin which in turn blocked the synaptic endocytosis. Dynasore worked as inhibitor of dynamin GTPase activity which blocks dynamin-dependent endocytosis not only in cells, but also including neurons.

体外研究

体内研究

激酶实验

细胞实验

动物实验

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Macia E, et al. Dev Cell, 2006, 10(6), 839-850.
[2] Thompson, H.M, et al. 2006. Nat. Chem. Biol. 2: 355-356.
[3] Newton, A.J., et al. 2006. Proc. Natl. Acad. Sci. U.S.A. 103: 17955-17960.
[4] Nankoe, S.R., et al. 2006. Trends Cell Biol. 16: 607-609.
[5] Young, A., et al. 2009. Biochem. J. 421: 377-385.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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