BIO1211

Research use only, not for human use.

BIO1211 (BIO-1211) is a potent, highly specific integrin α4β1 (VLA-4) inhibitor with Kd/IC50 of 20 pM/4 nM for the activated form of α4β1.

BIO1211 (BIO-1211) is a potent, highly specific integrin α4β1 (VLA-4) inhibitor with Kd/IC50 of 20 pM/4 nM for the activated form of α4β1; displays >200-fold selectivity over a range of other integrins (IC50 >100 uM for α1β1, α5β1 and α6β1), and reacts only with activated VLA4; inhibits ovalbumin-induced lung inflammation in vivo.

BIO-1211 almostly exhibits no activity for α1β1, α5β1, α6β1, αLβ2 and αIIbβ3.

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.

BIO-1211 | BIO 1211

Cell Cycle/DNA Damage

Integrin

Integrin

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187735-94-0

708.813

C36H48N6O9

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (352.71 mM)

O=C(O)[C@H]1N(C([C@H](C(C)C)NC([C@H](CC(O)=O)NC([C@H](CC(C)C)NC(CC2=CC=C(NC(NC3=CC=CC=C3C)=O)C=C2)=O)=O)=O)=O)CCC1

L-Proline, N-[[4-[[[(2-methylphenyl)amino]carbonyl]amino]phenyl]acetyl]-L-leucyl-L-a-aspartyl-L-valyl- (9CI)

(-20℃)

With Ice Pack

≥ 2 years