SCH79797 dihydrochloride

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1216720-69-2

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

SCH79797 dihydrochloride 是一种高效的选择性非肽蛋白酶激活受体 1 (PAR1) 拮抗剂。SCH79797 dihydrochloride 抑制高亲和力的凝血酶受体激活肽与PAR1的结合，IC₅₀值为 70 nM，K_i为 35 nM。SCH79797 dihydrochloride 以IC₅₀为 3 μM 抑制凝血酶诱导的血小板凝集。SCH79797 dihydrochloride 具有抗增殖和促凋亡作用，并限制了大鼠心脏的心肌缺血/再灌注损伤。SCH79797 dihydrochloride 还可以有效地阻止血管平滑肌细胞，内皮细胞和星形胶质细胞中的PAR1活化。

生物活性

SCH79797 dihydrochloride is a highly potent, selective nonpeptideprotease activated receptor1 (PAR1)antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinitythrombinreceptor-activating peptide toPAR1with anIC₅₀of 70 nM and aK_iof 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with anIC₅₀of 3 μM. SCH79797 dihydrochloride has antiproliferative andpro-apoptoticeffects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently preventsPAR1activation in vascular smooth muscle cells, endothelial cells, and astrocytes^[1]^[2]^[3]^[4].

IC₅₀& Target

Protease activated receptor 1 (PAR1)^[1]; Apoptosis^[3]

体外研究
(In Vitro)

SCH79797 inhibits high-affinity thrombin receptor-activating peptide ([³H]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 Ca²⁺concentration ([Ca²⁺]_i) in hCASMC. SCH79797 effectively inhibits this increase in [Ca²⁺]_i. SCH79797 completely inhibits Thrombin- and TK-stimulated [³H]thymidine incorporation^[1].
SCH79797 is able to interfere with the growth of several human and mouse cell lines, in a concentration-dependent manner. The ED₅₀for 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^[2].

体内研究
(In Vivo)

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^[4].

Animal Model:	Male Sprague Dawley rats (8 weeks of age) with myocardial I/R injury^[4]
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.

分子量

444.40

性状

Solid

Formula

C₂₃H₂₇Cl₂N₅

CAS 号

1216720-69-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 22 mg/mL(49.50 mM;Need ultrasonic and warming)

Ethanol : 11 mg/mL(24.75 mM;Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.2502 mL	11.2511 mL	22.5023 mL
5 mM	0.4500 mL	2.2502 mL	4.5005 mL
10 mM	0.2250 mL	1.1251 mL	2.2502 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。