172927-65-0

中文名称化合物 T28775

英文名称 Sibrafiban

CAS 172927-65-0

分子式 C20H28N4O6

分子量 420.46

MOL 文件 172927-65-0.mol

更新日期 2023/03/20 15:41:23

172927-65-0 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T28775

英文别名

Sibrafiban
WBNUCLPUOSXSNJ-UHFFFAOYSA-N
Acetic acid, 2-[[1-[(2S)-2-[[4-[(Z)-amino(hydroxyimino)methyl]benzoyl]amino]-1-oxopropyl]-4-piperidinyl]oxy]-, ethyl ester

物理化学性质

密度1.33±0.1 g/cm3(Predicted)

储存条件-20°C储存

溶解度DMSO : 33.33 mg/mL (79.27 mM; Need ultrasonic)

酸度系数(pKa)13.16±0.10(Predicted)

形态Solid

颜色White to off-white

常见问题列表

生物活性

Sibrafiban (RO 48-3657) 是一种 Ro 44-3888 的具有口服活性的，非肽，双重前药，是一种选择性的糖蛋白 IIb/IIIa 受体 (glycoprotein IIb/IIIa receptor) 拮抗剂。Sibrafiban 可抑制血小板聚集。

靶点

Glycoprotein IIb/IIIa receptor

体外研究

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.

体内研究

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.