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SCH79797 2HCl

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Chemical Structure| 1216720-69-2 同义名 : SCH 79797 (hydrochloride);SCH79797 dihydrochloride
CAS号 : 1216720-69-2
货号 : A788997
分子式 : C23H27Cl2N5
纯度 : 98%
分子量 : 444.4
MDL号 : MFCD04039788
存储条件:

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 20 mg/mL(45 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 10 mg/mL(22.5 mM),配合低频超声,并水浴加热至45℃助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方:
生物活性
描述 SCH79797 dihydrochloride is a highly potent and selective nonpeptide protease activated receptor 1 (PAR1) antagonist. It inhibits the binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride also inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. Moreover, it has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. Additionally, SCH79797 dihydrochloride potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes[1][2][3][4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.23mL

11.25mL

2.25mL

1.13mL

22.50mL

4.50mL

2.25mL

参考文献

[1]Ahn HS, et al. Inhibition of cellular action of thrombin by N3-cyclopropyl-7-[[4-(1-methylethyl)phenyl]methyl]-7H-pyrrolo[3, 2-f]quinazoline-1,3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonist. Biochem Pharmacol. 2000 Nov 15;60(10):1425-34.

[2]Di Serio C, et al. Protease-activated receptor 1-selective antagonist SCH79797 inhibits cell proliferation and induces apoptosis by a protease-activated receptor 1-independent mechanism. Basic Clin Pharmacol Toxicol. 2007 Jul;101(1):63-9.

[3]Sokolova E, et al. A novel therapeutic target in various lung diseases: airway proteases and protease-activated receptors. Pharmacol Ther. 2007 Jul;115(1):70-83.

[4]Strande JL, et al. SCH 79797, a selective PAR1 antagonist, limits myocardial ischemia/reperfusion injury in rat hearts. Basic Res Cardiol. 2007 Jul;102(4):350-8.