1. Cytoskeleton
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  3. BIO5192

BIO5192 

Cat. No.: HY-107589
Handling Instructions

IC50: 1.8 nM (α4β1), 138 nM (α9β1), 1053 nM (α2β1), >500 nM (α4β7), >10000 nM (α11bβ3)

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.

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BIO5192 Chemical Structure

BIO5192 Chemical Structure

CAS No. : 327613-57-0

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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].

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. BIO5192 (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.
Molecular Weight

817.78

Formula

C₃₈H₄₆Cl₂N₆O₈S

CAS No.

327613-57-0

SMILES

O=[S](N(CCC1)[[email protected]@H]1C(N[[email protected]](C(O)=O)CCNC([[email protected]](CC(C)C)N(C)C(CC(C=C2)=CC=C2NC(NC(C=CC=C3)=C3C)=O)=O)=O)=O)(C4=CC(Cl)=CC(Cl)=C4)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

BIO5192BIO 5192BIO-5192IntegrinselectivehematopoieticstemprogenitorsmobilizationinflammatoryInhibitorinhibitorinhibit

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BIO5192
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HY-107589
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