Art. -Nr.: HY-14126

BIO-1211

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

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.

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Reinheit: 99.64%
CAS. Nr.: 187735-94-0
Formel: C₃₆H₄₈N₆O₉
Molecular Weight:708.80

Speicherung:

Sealed storage, away from moisture.

Powder -80°C, 2 years , -20°C, 1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

BIO-1211 Chemical Structure

CAS. Nr.: 187735-94-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]^[2]^[3].

IC₅₀ & Target^[3]

α4β1

4 nM (IC₅₀)

α4β7

2 μM (IC₅₀)

Alle Integrin Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	<0.5 nM Compound: Bio-1211	Inhibition of VLA-4 receptor expressed in CHO cells Inhibition of VLA-4 receptor expressed in CHO cells	[PMID: 15582407]
Jurkat	IC₅₀	0.13 nM Compound: BIO-1211	Antagonistic activity against VLA-4 integrin of human jurkat cells using [125I]VCAM-Ig as radioligand Antagonistic activity against VLA-4 integrin of human jurkat cells using [125I]VCAM-Ig as radioligand	[PMID: 11591507]
Jurkat	IC₅₀	0.13 nM Compound: 2	Inhibition of [125I]VCAM-Ig binding to Alpha-4 beta-1 (VLA-4) of Jurkat cells Inhibition of [125I]VCAM-Ig binding to Alpha-4 beta-1 (VLA-4) of Jurkat cells	[PMID: 11844701]
Jurkat	IC₅₀	0.3 nM Compound: BIO-1211	Inhibition of Integrin alpha-4-beta-1-mediated adhesion in human jurkat cells Inhibition of Integrin alpha-4-beta-1-mediated adhesion in human jurkat cells	[PMID: 16767086]
Jurkat	IC₅₀	4 nM Compound: 12	Inhibition of integrin alpha4-beta1 adhesion to Jurkat cells Inhibition of integrin alpha4-beta1 adhesion to Jurkat cells	[PMID: 10072689]
Jurkat	IC₅₀	4.8 nM Compound: 1, BIO1211, MPUPA-LDVP-OH	Displacement of [125I]-FN from human alpha4beta1 integrin expressed in human Jurkat cells by scintillation proximity assay Displacement of [125I]-FN from human alpha4beta1 integrin expressed in human Jurkat cells by scintillation proximity assay	[PMID: 24412498]
Jurkat	IC₅₀	7.6 nM Compound: 1, BIO1211, MPUPA-LDVP-OH	Inhibition of human alpha4beta1 integrin expressed in human Jurkat cells assessed as inhibition of cell adhesion to VCAM-1 Inhibition of human alpha4beta1 integrin expressed in human Jurkat cells assessed as inhibition of cell adhesion to VCAM-1	[PMID: 24412498]
Jurkat	IC₅₀	7.6 nM Compound: BIO1211	Inhibition of human alpha4beta1 integrin expressed in human Jurkat cells assessed as inhibition of cell adhesion to VCAM-1 Inhibition of human alpha4beta1 integrin expressed in human Jurkat cells assessed as inhibition of cell adhesion to VCAM-1	[PMID: 26101577]
JY	IC₅₀	>100 μM Compound: 12	Inhibition of ICAM-1 transfected CHO cell adhesion to integrin alphaL-beta2 of human JY cells Inhibition of ICAM-1 transfected CHO cell adhesion to integrin alphaL-beta2 of human JY cells	[PMID: 10072689]
JY	IC₅₀	2 μM Compound: 12	Inhibition of integrin alpha4-beta7 adhesion to JY cells Inhibition of integrin alpha4-beta7 adhesion to JY cells	[PMID: 10072689]
K562	IC₅₀	>100 μM Compound: 12	Inhibition of integrin alpha1-beta1 adhesion using K562 cells expressing alpha-1 Inhibition of integrin alpha1-beta1 adhesion using K562 cells expressing alpha-1	[PMID: 10072689]
K562	IC₅₀	>100 μM Compound: 12	Inhibition of integrin alpha6-beta1 adhesion using K562 cells expressing alpha-6 Inhibition of integrin alpha6-beta1 adhesion using K562 cells expressing alpha-6	[PMID: 10072689]
K562	IC₅₀	>100 μM Compound: 12	Inhibition of integrin alpha5-beta1 adhesion to K562 cells Inhibition of integrin alpha5-beta1 adhesion to K562 cells	[PMID: 10072689]
RPMI-8866	IC₅₀	433 nM Compound: BIO-1211	Inhibition of [125I]VCAM-Ig binding to alpha4-beta7 integrin of human RPMI-8866 cells Inhibition of [125I]VCAM-Ig binding to alpha4-beta7 integrin of human RPMI-8866 cells	[PMID: 11591507]
RPMI-8866	IC₅₀	862 nM Compound: BIO-1211	Inhibition of [125I]MAdCAM-Ig binding to alpha4-beta7 integrin of human RPMI-8866 cells Inhibition of [125I]MAdCAM-Ig binding to alpha4-beta7 integrin of human RPMI-8866 cells	[PMID: 11591507]

In Vitro

BIO-1211 almostly exhibits no activity for α1β1, α5β1, α6β1, αLβ2 and αIIbβ3^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS. Nr. 187735-94-0
Appearance Solid
Molecular Weight 708.80
Formel C₃₆H₄₈N₆O₉
Color White to off-white
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (4)

All RT-PCRWBCell Proliferation/Viability AssayCell Imaging/Staining

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Journal Impact Factor

Acta Biomater

Laminin alpha 4 promotes bone regeneration by facilitating cell adhesion and vascularization. [Abstract]

2021 May:126:183-198. PMID: 33711525
Leukemia

Distinct stromal cell populations define the B-cell acute lymphoblastic leukemia microenvironment. [Abstract]

2025 Aug 15. PMID: 40817406

BIO-1211 purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Aug 15. [Abstract]

Effect of cytokine signaling blockade on ALL cell survival in co-culture with stromal populations. ALL cells were co-cultured with early mesenchymal progenitors, adipogenic progenitors, or cultured alone. Effect of VCAM1 blockade on ALL cell viability in co-culture or monoculture. Effect of blocking integrin beta 1 (ITGB1) using a blocking antibody or the small peptidomimetic drug BIO-1211 (50 uM; 7 days), Mouse IgG1 kappa, Isotype Control (1 ug/mL; 7 days)on ALL cell viability in co-culture or monoculture.
Cell Rep Methods

Efficiency landscape of bioorthogonal click reactions producing bispecific antibody conjugates. [Abstract]

2026 Jun 15;6(6):101416. PMID: 42019503
Vascul Pharmacol

Midkine mediates dysfunction of liver sinusoidal endothelial cells through integrin α4 and α6. [Abstract]

2022 Dec:147:107113. PMID: 36184060

BIO-1211 purchased from MedChemExpress. Usage Cited in: Vascul Pharmacol. 2022 Dec:147:107113. [Abstract]

Different subtypes of integrin receptors lead to opposite trends in the effect of MK in regulating hepatic sinusoidal diastolic homeostasis. The effect of exogenous MK stimulation of Itgα4⁺ and Itgα6⁺ on NO, ET1, TXA2 expression and the reversal of NO, ET1, TXA2 expression by BIO1211 (4 nM in LSECs of Itgα4⁺; 100 μM in LSECs of Itgα6⁺) in LSECs.

BIO-1211 purchased from MedChemExpress. Usage Cited in: Vascul Pharmacol. 2022 Dec:147:107113. [Abstract]

The effect of exogenous MK stimulation of Itgα4+ and Itgα6+ and BIO1211 (4 nM in LSECs of Itgα4⁺; 100 μM in LSECs of Itgα6⁺) in LSECs. WB detection of CAV-1 and Akt/eNOS signaling pathway expression, n = 3.

BIO-1211 purchased from MedChemExpress. Usage Cited in: Vascul Pharmacol. 2022 Dec:147:107113. [Abstract]

The effect of exogenous MK stimulation of Itgα4⁺ and Itgα6⁺ and BIO1211 (4 nM in LSECs of Itgα4⁺; 100 μM in LSECs of Itgα6⁺) in LSECs. Immunofluorescence detection of CAV-1 expression in LSECs, Scale bar =100μm.

BIO-1211 purchased from MedChemExpress. Usage Cited in: Vascul Pharmacol. 2022 Dec:147:107113. [Abstract]

MK induces hepatic sinusoidal contraction through integrin α6 promoting Src/Shc pathway. WB detection of the expression of Src/Shc signaling pathway in cells, n=3. BIO-1211 (4 nM in LSECs of Itgα4⁺; 100 μM in LSECs of Itgα6⁺).

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (352.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4108 mL

7.0542 mL

14.1084 mL

5 mM

0.2822 mL

1.4108 mL

2.8217 mL

10 mM

0.1411 mL

0.7054 mL

1.4108 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (2.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (2.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (2.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[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. [Content Brief]

[3]. K c Lin, et al. Selective, tight-binding inhibitors of integrin alpha4beta1 that inhibit allergic airway responses. J Med Chem. 1999 Mar 11;42(5):920-34. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.4108 mL	7.0542 mL	14.1084 mL	35.2709 mL
	5 mM	0.2822 mL	1.4108 mL	2.8217 mL	7.0542 mL
	10 mM	0.1411 mL	0.7054 mL	1.4108 mL	3.5271 mL
	15 mM	0.0941 mL	0.4703 mL	0.9406 mL	2.3514 mL
	20 mM	0.0705 mL	0.3527 mL	0.7054 mL	1.7635 mL
	25 mM	0.0564 mL	0.2822 mL	0.5643 mL	1.4108 mL
	30 mM	0.0470 mL	0.2351 mL	0.4703 mL	1.1757 mL
	40 mM	0.0353 mL	0.1764 mL	0.3527 mL	0.8818 mL
	50 mM	0.0282 mL	0.1411 mL	0.2822 mL	0.7054 mL
	60 mM	0.0235 mL	0.1176 mL	0.2351 mL	0.5878 mL
	80 mM	0.0176 mL	0.0882 mL	0.1764 mL	0.4409 mL
	100 mM	0.0141 mL	0.0705 mL	0.1411 mL	0.3527 mL

Keywords

BIO-1211

4 Cited Publications

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BIO-1211

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Peptide Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Extracellular Vesicles (EVs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Peptide Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) BIO-1211

Alle Integrin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BIO-1211

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Peptide Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Extracellular Vesicles (EVs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Peptide Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) BIO-1211

Alle Integrin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BIO-1211 Related Classifications

HY-14126 Related Classifications