产品
编 号:F234870
分子式:C36H48N6O9
分子量:708.8
产品类型
结构图
CAS No: 187735-94-0
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产品详情
生物活性:
BIO-1211 is a highly selective and orally active α4β1 (VLA-4) inhibitor, with IC50 values of 4 nM and 2 μM for α4β1 and α4β7, respectively.
体内研究:
BIO-1211 (5 and 10 mg/kg, orally, once every other day) results in reduced cytokines expression, leukocyte trafficking, and inhibition of inflammatory responses in EAE in a dose-independent manner. BIO-1211 exhibits 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.Animal Model:Naive, C57BL/6 mice (male, 8 weeks old, 20-25 g weight).
Dosage:5 and 10 mg/kg.
Administration:Orally once every other day starting the day before immunization until day 21 post-immunization.
Result:Could prevent the induction of EAE.Significantly delayed the onset of EAE and reduced the severity of clinical EAE compared to the vehicle group.Markedly reduced the expression of both CD11b and CD45 in comparison with the vehicle group.mRNA and soluble form of a subset of target inflammatory cytokines (IFNγ, IL-17, and TNF-α) was dramatically decreased.
体外研究:
BIO-1211 almostly exhibits no activity for α1β1, α5β1, α6β1, αLβ2 and αIIbβ3.