172927-65-0

172927-65-0 structure

Name: Sibrafiban
Chemical Name: ethyl 2-[1-[(2S)-2-[[4-[(Z)-N'-hydroxycarbamimidoyl]benzoyl]amino]propanoyl]piperidin-4-yl]oxyacetate
CAS Number: 172927-65-0
Molecular Formula: C₂₀H₂₈N₄O₆
Molecular Weight: 420.46000
Catalog: Signaling Pathways Cytoskeleton Integrin
Create Date: 2016-12-06 10:40:38
Modify Date: 2024-01-15 19:31:26
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].

Name	ethyl 2-[1-[(2S)-2-[[4-[(Z)-N'-hydroxycarbamimidoyl]benzoyl]amino]propanoyl]piperidin-4-yl]oxyacetate
Synonyms	Xubix UNII-YUE443B0NF Sibrafiban Ro 48-3657

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].
Related Catalog	Research Areas >> Cardiovascular Disease Signaling Pathways >> Cytoskeleton >> Integrin
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].
References	[1]. M Dooley, et al. Sibrafiban. Drugs. 1999 Feb;57(2):225-30; discussion 231-2. [2]. B Wittke, et al. Pharmacokinetics and pharmacodynamics of sibrafiban alone or in combination with ticlopidine and aspirin. Br J Clin Pharmacol. 2000 Mar;49(3):231-9. [3]. Jeffrey T Billheimer, et al. Effects of glycoprotein IIb/IIIa antagonists on platelet activation: development of a transfer method to mimic peak to trough receptor occupancy. Thromb Res. 2002 Sep 15;107(6):303-17.

Density	1.33g/cm3
Molecular Formula	C₂₀H₂₈N₄O₆
Molecular Weight	420.46000
Exact Mass	420.20100
PSA	143.55000
LogP	1.49920
Index of Refraction	1.598

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