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Sibrafiban (Synonyms: RO 48-3657)

Cat. No.: HY-10309
Handling Instructions

Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.

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

Sibrafiban Chemical Structure

Sibrafiban Chemical Structure

CAS No. : 172927-65-0

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Description

Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation[1][2][3].

IC50 & Target

Glycoprotein IIb/IIIa receptor[1]

In Vitro

The effects of site occupancy by Sibrafiban on platelet activation are assessed using P-selectin expression, fibrinogen binding and microaggregate formation. Sibrafiban inhibits ADP and TRAP-stimulated fibrinogen binding and microaggregate formation in a concentration-dependent manner, whereas P-selectin expression is relatively unaltered. A decrease in site occupancy from peak to trough of Sibrafiban does not result in increased activation of platelets[3].

In Vivo

The effects of Ro 44-3888 on the platelet aggregation response to ADP (17 μmol) and on cutaneous bleeding times is determined in 8 rhesus monkeys given Sibrafiban 0.25 mg/kg/day or 0.5 mg/kg/day orally for 8 days. The maximum inhibition of ex vivo platelet aggregation and prolongation of bleeding time by Ro 44-3888 are dose dependent[1].

Molecular Weight

420.46

Formula

C₂₀H₂₈N₄O₆

CAS No.

172927-65-0

SMILES

O=C(OCC)COC1CCN(C([[email protected]@H](NC(C2=CC=C(/C(N)=N/O)C=C2)=O)C)=O)CC1.[(Z)]

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Storage

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

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Keywords:

SibrafibanRO 48-3657IntegrinRo 44-3888orallynonpeptidedouble-prodrugglycoprotein-IIbglycoprotein-IIIaantiplateletInhibitorinhibitorinhibit

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