生物活性

TH-237A(meso-GS 164)是神经保护剂，有很好的血脑屏障渗透性。TH-237A was investigated for effectiveness in protecting neurons against several toxic stimuli and its interaction with the microtubule network. In vitro studies using bovine brain microvessel endothelial cells experiments and in situ brain perfusion studies suggested that TH-237A can readily cross the blood-brain barrier in a passive manner. Chronic treatment of P301L mutant Tau mice with TH-237A led to a reduction of abnormal Tau in brain and spinal cord. The results suggest that this small, brain permeable compound may provide a lead structure for development of new therapeutic approaches to neurofibrillary pathology. Exposure of neuronal cultures to Aβ peptide in the presence of 5 nM TH-237A resulted in a 50% increase in survival. Neuronal cultures treated with other toxic stimuli such as staurosporine, thapsigargin, paraquat and H2O2 showed significantly enhanced survival in the presence of TH-237A. Microtubule binding and tubulin assembly studies revealed differences compared to paclitaxel, but confirmed the interaction of TH-237A with microtubules. Furthermore, in vitro studies using bovine brain microvessel endothelial cells experiments suggest that TH-237A can readily cross the blood-brain barrier in a passive manner.

化学数据

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，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

储备液配制

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。