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1216720-69-2

中文名稱 SCH79797 DIHYDROCHLORIDE
英文名稱 7H-Pyrrolo[3,2-f]quinazoline-1,3-diaMine, N3-cyclopropyl-7-[[4-(1-Methylethyl)phenyl]Methyl]-, (Hydrochloride) (1:2)
CAS 1216720-69-2
分子式 C23H25N5
分子量 371.478
MOL 文件 1216720-69-2.mol
更新日期 2024/12/23 10:32:57
1216720-69-2 結(jié)構(gòu)式 1216720-69-2 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12870
化合物SCH79797 DIHYDROCHLORIDE
N3- 環(huán)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 - 二胺鹽酸鹽 (1:2)
英文別名
SCH 79797 (hydrochloride)
7H-Pyrrolo[3,2-f]quinazoline-1,3-diaMine, N3-cyclopropyl-7-[[4-(1-Methylethyl)phenyl]Methyl]-, (Hydrochloride) (1:2)

物理化學(xué)性質(zhì)

儲存條件Store at 2-8°C, protect from light
溶解度Soluble to 25 mM in ethanol and to 50 mM in DMSO
形態(tài)粉末
顏色White to yellow

常見問題列表

生物活性
SCH79797 dihydrochloride 是一種高效的選擇性非肽蛋白酶激活受體 1 (PAR1) 拮抗劑。SCH79797 dihydrochloride 抑制高親和力的凝血酶受體激活肽與 PAR1 的結(jié)合,IC50 值為 70 nM,Ki 為 35 nM。SCH79797 dihydrochloride 以 IC50 為 3 μM 抑制凝血酶誘導(dǎo)的血小板凝集。SCH79797 dihydrochloride 具有抗增殖和促凋亡作用,并限制了大鼠心臟的心肌缺血/再灌注損傷。SCH79797 dihydrochloride 還可以有效地阻止血管平滑肌細(xì)胞,內(nèi)皮細(xì)胞和星形膠質(zhì)細(xì)胞中的 PAR1 活化。
靶點

Protease activated receptor 1 (PAR1); Apoptosis

體外研究

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.

體內(nèi)研究

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.
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