BIO-1211 是高度选择性的、口服有效的α4β1 (VLA-4)抑制剂,对 α4β1 和 α4β7 的IC50分别为 4 nM 和 2 μM。
产品描述
BIO-1211 is a more potent inhibitor of α4β1 (VLA-4, IC50 = 4 nM) over α4β7(IC50 = 2 μM).
体外活性
BIO-1211 does not show activity against α1β1, α5β1, α6β1, αLβ2 and αIIbβ3[2].
体内活性
In naive, C57BL/6 mice, BIO-1211 exhibited a considerable depletion in the EAE clinical score, which correlated with decreased expression of TNF-α, IL-17, IFN-γ and pervade of CD11b+ and CD45+ cells into the cerebral cortex. BIO-1211 resulted in reduced cytokines expression, leukocyte trafficking, and inhibition of inflammatory responses in a dose-independent manner[1].
Cas No.
187735-94-0
分子式
C36H48N6O9
分子量
708.80
储存和溶解度
DMSO:250 mg/mL (352.71 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years