BIO 5192

Modify Date: 2024-01-24 14:00:32

BIO 5192 Structure
BIO 5192 structure
Common Name BIO 5192
CAS Number 327613-57-0 Molecular Weight 817.778
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C38H46Cl2N6O8S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of BIO 5192


BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 μM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2].

 Names

Name BIO-5192
Synonym More Synonyms

 BIO 5192 Biological Activity

Description BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 μM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2].
Related Catalog
In Vivo The combination of BIO5192 (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1]. BIO5192 (30 mg/kg; s.c; bid; during days 5 through 14) delays paralysis associated with EAE (experimental autoimmune encephalomyelitis)[2]. BIO5192 (1 mg/kg, i.v.) shows the terminal half-life is 1.1 h. IO5192 (3, 10, and 30 mg/kg; s.c.) shows half-lives of 1.7, 2.7, and 4.7 h, respectively. The blood plasma curves show that the AUC for the s.c. route of administration increased about 2.5-fold from 5,460 h*ng/ml for the 3 mg/kg dose to 14,175 h*ng/ml for the 30 mg/kg[1]. Animal Model: C57BL/6J x 129Sv/J F1 mice[1] Dosage: 1 mg/kg (with Plerixafor: 5 mg/kg) Administration: I.v. Result: Exerted an additive effect on progenitor mobilization. Animal Model: Healthy female Lewis rats weighing 150g[2] Dosage: 30 mg/kg Administration: S.c; bid; during days 5 through 14 Result: Showed a 3-day delay in onset of disease.
References

[1]. Ramirez P, et al. BIO5192, a small molecule inhibitor of VLA-4, mobilizes hematopoietic stem and progenitor cells. Blood. 2009;114(7):1340‐1343.

[2]. Leone DR, et al. An assessment of the mechanistic differences between two integrin alpha 4 beta 1 inhibitors, the monoclonal antibody TA-2 and the small molecule BIO5192, in rat experimental autoimmune encephalomyelitis. J Pharmacol Exp Ther. 2003;305(3):1150‐1162.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Molecular Formula C38H46Cl2N6O8S
Molecular Weight 817.778
Exact Mass 816.247498
LogP 5.10
Index of Refraction 1.625

 Synonyms

(2S)-2-({1-[(3,5-Dichlorophenyl)sulfonyl]-L-prolyl}amino)-4-({N-methyl-N-[(4-{[(2-methylphenyl)carbamoyl]amino}phenyl)acetyl]-L-leucyl}amino)butanoic acid
MFCD26408178
55W0N209OS
Butanoic acid, 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]-, (2S)-
BIO-5192
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  • Product Name: BIO-5192
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  • Purity: 98.0%
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