2. GPCR/G Protein Apoptosis
  3. Protease Activated Receptor (PAR) Apoptosis
  4. SCH79797 dihydrochloride

SCH79797 dihydrochloride 

目录号: HY-14994 纯度: 99.91%
COA 产品使用指南

摩尔计算器

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，Ki 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。

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SCH79797 dihydrochloride Chemical Structure

SCH79797 dihydrochloride Chemical Structure

CAS No. : 1216720-69-2

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规格 价格 是否有货 数量
5 mg ￥1300
In-stock
10 mg ￥1900
In-stock
25 mg ￥4100
In-stock
50 mg ￥7200
In-stock
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200 mg   询价  

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Customer Review

Other Forms of SCH79797 dihydrochloride:

SCH79797 dihydrochloride 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits 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 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation 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 ED50 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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SCH79797 dihydrochloride 相关抗体:
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C23H27Cl2N5
CAS 号
性状

固体

颜色

White to yellow

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 中的溶解度 : 22 mg/mL (49.50 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

Ethanol 中的溶解度 : 11 mg/mL (24.75 mM; 超声加热助溶)

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
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.91%

COA (269 KB) LCMS (267 KB) 元素分析报告 (215 KB)

产品使用指南 (1538 KB)
参考文献

SCH79797 dihydrochloride 相关分类

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.2502 mL 11.2511 mL 22.5023 mL 56.2556 mL
5 mM 0.4500 mL 2.2502 mL 4.5005 mL 11.2511 mL
10 mM 0.2250 mL 1.1251 mL 2.2502 mL 5.6256 mL
15 mM 0.1500 mL 0.7501 mL 1.5002 mL 3.7504 mL
20 mM 0.1125 mL 0.5626 mL 1.1251 mL 2.8128 mL
DMSO 25 mM 0.0900 mL 0.4500 mL 0.9001 mL 2.2502 mL
30 mM 0.0750 mL 0.3750 mL 0.7501 mL 1.8752 mL
40 mM 0.0563 mL 0.2813 mL 0.5626 mL 1.4064 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SCH797971216720-69-2SCH 79797SCH-79797Protease Activated Receptor (PAR)ApoptosisThrombin receptorsNonpeptidethrombinplateletsPAR1cardioprotectionthrombosiswortmannininfarctantiproliferativepro-apoptoticInhibitorinhibitorinhibit

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SCH79797 dihydrochloride
目录号：
HY-14994
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