生物活性

Vedolizumab是一种全人源化单克隆抗体，特异性拮抗α4β7整合素，抑制α4β7整合素对肠道黏膜细胞粘附分子MAdCAM-1的结合。Vedolizumab blocks the α4β7 integrin, results in gut-selective anti-inflammatory activity. Vedolizumab binds to memory CD4(+) T ａnd B lymphocytes with subnanomolar potency (EC(50) = 0.3-0.4 nM). Vedolizumab also binds to eosinophils at high levels, ａnd to naive T-helper lymphocytes, naive ａnd memory cytotoxic T lymphocytes, B lymphocytes, natural killer cells, ａnd basophils at lower levels. Vedolizumab selectively inhibits adhesion of alpha(4)beta(7)-expressing cells to mucosal addressin cell adhesion molecule 1 (median inhibition concentration [IC(50)] = 0.02-0.06 microg/ml) ａnd fibronectin (IC(50) = 0.02 microg/ml), but not vascular cell adhesion molecule 1.

化学性质

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液，需考虑其在不同溶剂中的溶解度限制。

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

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Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Fedyk ER, et al. Inflamm Bowel Dis. Exclusive antagonism of the α4 β7 integrin by vedolizumab confirms the gut-selectivity of this pathway in primates.

[2] Soler D, et al. J Pharmacol Exp Ther. The binding specificity ａnd selective antagonism of vedolizumab, an anti-alpha4beta7 integrin therapeutic antibody in development for inflammatory bowel diseases.