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BIO5192 hydrate 

Cat. No.: HY-107589A Purity: >98.0%
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BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.

For research use only. We do not sell to patients.

BIO5192 hydrate Chemical Structure

BIO5192 hydrate Chemical Structure

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Description

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

IC50 & Target[1]

α4β1

1.8 nM (IC50)

α9β1

138 nM (IC50)

α2β1

1053 nM (IC50)

α4β7

>500 nM (IC50)

In Vivo

The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1].
BIO5192 hydrate (30 mg/kg; s.c; bid; during days 5 through 14) delays paralysis associated with EAE (experimental autoimmune encephalomyelitis)[2].
BIO5192 hydrate (1 mg/kg, i.v.) shows the terminal half-life is 1.1 hours. BIO5192 hydrate (3, 10, and 30 mg/kg; s.c.) shows half-lives of 1.7, 2.7, and 4.7 hours, 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

835.79

Formula

C₃₈H₄₈Cl₂N₆O₉S

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.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >98.0%

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Keywords:

BIO5192BIO 5192BIO-5192IntegrinselectivehematopoieticstemprogenitorsmobilizationinflammatoryInhibitorinhibitorinhibit

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Product Name:
BIO5192 hydrate
Cat. No.:
HY-107589A
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