BIO 1211;BIO-1211;(4-((2-Methylphenyl)aminocarbonyl)-aminophenyl)acetyl-Fibronectin CS-1 Fragment (1980-1983);(4-((2-METHYLPHENYL)AMINOCARBONYL)-AMINOPHENYL)ACETYL-LEU-ASP-VAL-PRO-OH
Cas No.
187735-94-0
分子式
C36H48N6O9
分子量
708.80
包装储存
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
BIO-1211 is a highly selective and orally active α4β1 (VLA-4) inhibitor, with IC 50 values of 4 nM and 2 μM for α4β1 and α4β7, respectively.
性状
Solid
IC50 & Target[1][2]
α4β1 4 nM (IC50) α4β7 2 μM (IC50
体外研究(In Vitro)
BIO-1211 almostly exhibits no activity for α1β1, α5β1, α6β1, αLβ2 and αIIbβ3. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
参考文献
[1]. L L Chen, et al. Multiple activation states of integrin alpha4beta1 detected through their different affinities for a small molecule ligand. J Biol Chem. 1999 May 7;274(19):13167-75.[2]. Nourollah Ramroodi, et al. Prophylactic Effect of BIO-1211 Small-Molecule Antagonist of VLA-4 in the EAE Mouse Model of Multiple Sclerosis. Immunol Invest. 2015;44(7):694-712.
溶解度数据
In Vitro: DMSO : 250 mg/mL (352.71 mM; Need ultrasonic)配制储备液