BIO-1211
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.
For research use only. We do not sell to patients.
- Purity: 99.64%
- CAS No.: 187735-94-0
- Formula: C36H48N6O9
- Molecular Weight:708.80
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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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BIO-1211
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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RT-PCR
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WB
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Cell Imaging/Staining
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WB
Biological Activity
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α4β1 4 nM (IC50) |
α4β7 2 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
<0.5 nM
Compound: Bio-1211
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Inhibition of VLA-4 receptor expressed in CHO cells
Inhibition of VLA-4 receptor expressed in CHO cells
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[PMID: 15582407] |
| Jurkat | IC50 |
0.13 nM
Compound: BIO-1211
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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
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[PMID: 11591507] |
| Jurkat | IC50 |
0.13 nM
Compound: 2
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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
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[PMID: 11844701] |
| Jurkat | IC50 |
0.3 nM
Compound: BIO-1211
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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
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[PMID: 16767086] |
| Jurkat | IC50 |
4 nM
Compound: 12
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Inhibition of integrin alpha4-beta1 adhesion to Jurkat cells
Inhibition of integrin alpha4-beta1 adhesion to Jurkat cells
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[PMID: 10072689] |
| Jurkat | IC50 |
4.8 nM
Compound: 1, BIO1211, MPUPA-LDVP-OH
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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
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[PMID: 24412498] |
| Jurkat | IC50 |
7.6 nM
Compound: 1, BIO1211, MPUPA-LDVP-OH
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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
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[PMID: 24412498] |
| Jurkat | IC50 |
7.6 nM
Compound: BIO1211
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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
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[PMID: 26101577] |
| JY | IC50 |
>100 μM
Compound: 12
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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
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[PMID: 10072689] |
| JY | IC50 |
2 μM
Compound: 12
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Inhibition of integrin alpha4-beta7 adhesion to JY cells
Inhibition of integrin alpha4-beta7 adhesion to JY cells
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[PMID: 10072689] |
| K562 | IC50 |
>100 μM
Compound: 12
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Inhibition of integrin alpha1-beta1 adhesion using K562 cells expressing alpha-1
Inhibition of integrin alpha1-beta1 adhesion using K562 cells expressing alpha-1
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[PMID: 10072689] |
| K562 | IC50 |
>100 μM
Compound: 12
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Inhibition of integrin alpha6-beta1 adhesion using K562 cells expressing alpha-6
Inhibition of integrin alpha6-beta1 adhesion using K562 cells expressing alpha-6
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[PMID: 10072689] |
| K562 | IC50 |
>100 μM
Compound: 12
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Inhibition of integrin alpha5-beta1 adhesion to K562 cells
Inhibition of integrin alpha5-beta1 adhesion to K562 cells
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[PMID: 10072689] |
| RPMI-8866 | IC50 |
433 nM
Compound: BIO-1211
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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
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[PMID: 11591507] |
| RPMI-8866 | IC50 |
862 nM
Compound: BIO-1211
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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
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[PMID: 11591507] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Naive, C57BL/6 mice (male, 8 weeks old, 20-25 g weight)[2].
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Dosage:5 and 10 mg/kg.
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Administration:Orally once every other day starting the day before immunization until day 21 post-immunization.
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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
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CAS No. 187735-94-0
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Appearance Solid
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Molecular Weight 708.80
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Formula C36H48N6O9
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Color White to off-white
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
Publications (4)
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Journal Impact Factor
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Most Recent
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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.
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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+).
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (274 KB)
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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)
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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
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.
| 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
HY-14126 Related Classifications
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