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172927-65-0

中文名稱 化合物 T28775
英文名稱 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 結(jié)構(gòu)式 172927-65-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T28775
英文別名
Sibrafiban
WBNUCLPUOSXSNJ-UHFFFAOYSA-N
Acetic acid, 2-[[1-[(2S)-2-[[4-[(Z)-amino(hydroxyimino)methyl]benzoyl]amino]-1-oxopropyl]-4-piperidinyl]oxy]-, ethyl ester

物理化學(xué)性質(zhì)

密度1.33±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO : 33.33 mg/mL (79.27 mM; Need ultrasonic)
酸度系數(shù)(pKa)13.16±0.10(Predicted)
形態(tài)Solid
顏色White to off-white

常見問題列表

生物活性
Sibrafiban (RO 48-3657) 是一種 Ro 44-3888 的具有口服活性的,非肽,雙重前藥,是一種選擇性的糖蛋白 IIb/IIIa 受體 (glycoprotein IIb/IIIa receptor) 拮抗劑。Sibrafiban 可抑制血小板聚集。
靶點

Glycoprotein IIb/IIIa receptor

體外研究

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.

體內(nèi)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.

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