BIO-1211

Name: BIO-1211
Brand: MedChemExpress
SKU: HY-14126
Rating: 5.0 (3 reviews)

Cat. No.: HY-14126 Purity: 99.64%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

CAS No. : 187735-94-0

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE BIO-1211

RT-PCR

Cell Proliferation/Viability Assay

Cell Imaging/Staining

: 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.

: 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⁺).

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View All Isoforms

αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

Biological Activity
Purity & Documentation
References
Customer Review

Description

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)

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]
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]
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]
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	0.13 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	0.3 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]
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 alpha5-beta1 adhesion to K562 cells Inhibition of integrin alpha5-beta1 adhesion to K562 cells	[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]
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.

Molecular Weight

708.80

Formula

C₃₆H₄₈N₆O₉

CAS No.

187735-94-0

Appearance

Solid

Color

White to off-white

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.64%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (246 KB) RP-HPLC (264 KB) MS (70 KB) Elemental Analysis Report (105 KB)

Handling Instructions (2659 KB)

References

[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]

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

BIO-1211 Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BIO-1211187735-94-0BIO1211BIO 1211IntegrinInhibitorinhibitorinhibit

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BIO-1211

Customer Review

BIO-1211 Related Antibodies

3 Publications Citing Use of MCE BIO-1211

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•Related Screening Libraries:

•Related Small Molecules:

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View All Integrin Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

BIO-1211 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

BIO-1211 Related Classifications

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