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Submit ReviewBIO 5192
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)
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 |
| InChI Key | MNQBPRHHZPXCKZ-ZDCRTTOTSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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:
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
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
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.
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