BIO 5192

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Description: Highly potent and selective inhibitor of integrin α4β1 (VLA-4)
Chemical Name: (2S)-2-[[[(2S)-1-[(3,5-Dichlorophenyl)sulfonyl]-2-pyrrolidinyl]carbonyl]amino]-4-[[(2S)-4-methyl-2-[methyl[2-[4-[[[(2-methylphenyl)amino]carbonyl]amino]phenyl]acetyl]amino]-1-oxopentyl]amino]butanoic acid
Purity: ≥98% (HPLC)
Citations (3)
Reviews (1)
Literature (2)

Biological Activity for BIO 5192

BIO 5192 is a highly selective and potent inhibitor of integrin α4β1 (Very Late Antigen-4; VLA-4) (Kd < 10 pM). Selectively binds α4β1 over a range of other integrins (IC50 values are 1.8, 138, 1053, > 500 and > 10,000 nM for α4β1, α9β1, α2β1, α4β7 and αIIbβ3, respectively). Induces a 30-fold increase in mobilization of murine hematopoietic stem and progenitor cells; displays a 3-fold additive effect with AMD 3100 (Cat. No. 3299). Decreases oxidative damage and improves neurological function following spinal cord injury in rats.

Compound Libraries for BIO 5192

BIO 5192 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data for BIO 5192

M. Wt 817.78
Formula C38H46Cl2N6O8S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 327613-57-0
PubChem ID 10350459
Smiles O=C(NC2=CC=C(CC(N(C)[C@@H](CC(C)C)C(NCC[C@@H]([C@@](O)=O)N[C@]([C@H]3N(S(C4=CC(Cl)=CC(Cl)=C4)(=O)=O)CCC3)=O)=O)=O)C=C2)NC1=CC=CC=C1C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for BIO 5192

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 81.78 100

Preparing Stock Solutions for BIO 5192

The following data is based on the product molecular weight 817.78. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.22 mL 6.11 mL 12.23 mL
5 mM 0.24 mL 1.22 mL 2.45 mL
10 mM 0.12 mL 0.61 mL 1.22 mL
50 mM 0.02 mL 0.12 mL 0.24 mL

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Product Datasheets for BIO 5192

Certificate of Analysis / Product Datasheet
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References for BIO 5192

References are publications that support the biological activity of the product.

Leone et al (2003) An assessment of the mechanistic differences between two integrin α4β1 inhibitors, the monoclonal antibody TA-2 and the small molecule BIO5192, in rat experimental aut J.Pharmacol.Exp.Ther. 305 1150 PMID: 12626659

Xu et al (2008) A chemical approach to stem-cell biology and regenerative medicine. Nature 453 338 PMID: 18480815

Ramirez et al (2009) BIO5192, a small molecule inhibitor of VLA-4, mobilizes hematopoietic stem and progenitor cells. Blood. 1340 1340 PMID: 19571319

Bao et al (2008) An integrin inhibiting molecule decreases oxidative damage and improves neurological function after spinal cord injury. Exp.Neurol 214 160 PMID: 18926823

If you know of a relevant reference for BIO 5192, please let us know.

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3 Citations for BIO 5192

Citations are publications that use Tocris products. Selected citations for BIO 5192 include:

Jeff et al (2022) Differential CXCR4 expression on hematopoietic progenitor cells versus stem cells directs homing and engraftment. JCI Insight 7 PMID: 35531956

Narendiran et al (2020) HIFα independent mechanisms in renal carcinoma cells modulate divergent outcomes in fibronectin assembly mediated by hypoxia and CoCl2. Sci Rep 10 18560 PMID: 33122751

Takizawa (2017) Bone marrow-derived mesenchymal stem cells propagate immunosuppressive/anti-inflammatorymacrophages in cell-to-cell contact-independent and dependent manners under hypoxic culture. Exp Cell Res 358 441 PMID: 28712928

Do you know of a great paper that uses BIO 5192 from Tocris? Please let us know.

Reviews for BIO 5192

Average Rating: 5 (Based on 1 Review.)

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a4b1 conformation stabilizer.
By Martin Bush on 05/10/2018
Assay Type: In Vitro
Species: Human

We used this small molecule to lock a4b1 in an open conformation for EM imaging. It worked very nicely.

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Enabling Research By Provision of Chemical Tools Poster

Enabling Research By Provision of Chemical Tools Poster

The Tocris chemistry team has considerable chemistry knowledge and skill which it has recently been applying to the generation of new chemical probes from known tools and compounds to help answer biological questions. This poster presents some of the work carried out by Tocris scientists and focuses on two areas: the generation of libraries of chemical building blocks to support Degrader (PROTAC) research and the development of a fluorescent probe to study integrin biology. Presented at Chemical Tools for Complex Biological Systems II, 2019, Janelia Research Campus, USA.