1216720-69-2
1216720-69-2 结构式
基本信息
化合物SCH79797 DIHYDROCHLORIDE
N3- 环丙基- 7- [[4- (1- 甲基乙基) 苯基] 甲基] - 7H- 吡咯并[3, 2- F] 喹唑啉- 1, 3 - 二胺盐酸盐 (1:2)
7H-Pyrrolo[3,2-f]quinazoline-1,3-diaMine, N3-cyclopropyl-7-[[4-(1-Methylethyl)phenyl]Methyl]-, (Hydrochloride) (1:2)
物理化学性质
常见问题列表
Protease activated receptor 1 (PAR1); Apoptosis
SCH79797 inhibits high-affinity thrombin receptor-activating peptide ([
3
H]haTRAP) binding in a competitive manner. SCH79797 inhibits α-thrombin- and haTRAP-induced aggregation of human platelets, but does not inhibit human platelet aggregation induced by the tethered ligand agonist for protease-activated receptor-4 (PAR-4), γ-thrombin, ADP, or collagen. Thrombin produces transient increases in cytosolic free Ca
2+
concentration ([Ca
2+
]
i
) in hCASMC. SCH79797 effectively inhibits this increase in [Ca
2+
]
i
. SCH79797 completely inhibits Thrombin- and TK-stimulated [
3
H]thymidine incorporation .
SCH79797 is able to interfere with the growth of several human and mouse cell lines, in a concentration-dependent manner. The ED
50
for growth inhibition iss 75 nM, 81 nM and 116 nM for NIH 3T3, HEK 293 and A375 cells, respectively. In NIH 3T3 cells, SCH79797 inhibits serum-stimulated activation of p44/p42 mitogen-activated protein kinases (MAPK) at low concentrations and induces apoptosis at higher concentrations.
SCH79797 (2.5-250 μg/kg; intravenous injection; male Sprague Dawley rats) treatment immediately before or during ischemia reduces myocardial necrosis following I/R in the intact rat heart in two rat models of myocardial ischemia/reperfusion (I/R) injury. This response is dose-dependent with the optimal dose being 25 μg/kg.
| Animal Model: | Male Sprague Dawley rats (8 weeks of age) with myocardial I/R injury |
| Dosage: | 2.5 μg/kg, 10 μg/kg, 25 μg/kg, 50 μg/kg, 100 μg/kg, and 250 μg/kg |
| Administration: | Intravenous injection |
| Result: | Immediately before or during ischemia reduced myocardial necrosis following I/R in the intact rat heart. |