BIO 5192

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Cat.No. 5051 - BIO 5192 | C38H46Cl2N6O8S | CAS No. 327613-57-0
Description: Highly potent and selective inhibitor of integrin α4β1
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)
Datasheet
Citations (1)
Reviews (2)
Literature

Biological Activity

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

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Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 81.78 100
1eq. NaOH 40.89 50

Preparing Stock Solutions

The following data is based on the product molecular weight 817.78. Batch specific molecular weights may vary from batch to batch due to solvent 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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References

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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View all Integrin Inhibitors

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1 Citation 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


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Reviews for BIO 5192

Average Rating: 4.5 (Based on 2 Reviews.)

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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.


In Vivo alpha4 blockade
By Anonymous on 12/22/2017
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: Peripheral blood, Brain, spleen

BIO5192 was administered 10mg/kg daily.

Reconstituted in DMSO. Diluted for use in PBS. Clinical saline caused precipitation.


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