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  3. BIO-1211

BIO-1211 

目录号: HY-14126
产品使用指南

BIO-1211 是高度选择性的 α4β1 (VLA-4) 抑制剂,其对 α4β1 和 α4β7 的IC50 值分别为 4 nM 和2 μM。

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BIO-1211 Chemical Structure

BIO-1211 Chemical Structure

CAS No. : 187735-94-0

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Description

BIO-1211 is a high selective α4β1 (VLA-4) inhibitor, with IC50 values of 4 nM and 2 μM for α4β1 and α4β7, respectively[1][2][3].

IC50 & Target[3]

α4β1

4 nM (IC50)

α4β7

2 μM (IC50)

α1β1

>100 μM (IC50)

α5β1

>100 μM (IC50)

α6β1

>100 μM (IC50)

αLβ2

>100 μM (IC50)

αIIbβ3

>100 μM (IC50)

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[2].

Animal Model: Naive, C57BL/6 mice (male, 8 weeks old, 20-25 g weight)[2].
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.
Molecular Weight

708.80

Formula

C₃₆H₄₈N₆O₉

CAS No.

187735-94-0

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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The molarity calculator equation

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

BIO-1211BIO1211BIO 1211IntegrinInhibitorinhibitorinhibit

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产品名称:
BIO-1211
目录号:
HY-14126
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