中文名称: SCH79797 dihydrochloride
英文名称: SCH79797 dihydrochloride
CAS No: 1216720-69-2
分子式: C23H27Cl2N5
分子量: 444.4
S10692 SCH79797 dihydrochloride ≥98% (psaitong)
包装规格:
1mg 5mg 10mg 10mg 25mg 100mg in glass bottle
溶解性:
溶于DMSO(22 mg/mL 超声,加热)
产品描述:

基本信息

产品编号:

S10692 

产品名称:

SCH79797 dihydrochloride

CAS:

1216720-69-2

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C23H27Cl2N5

溶于液体

-80℃

6个月

分子量:

444.40

-20℃

1个月

化学名: 

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-1,3-二胺双盐酸盐N3-Cyclopropyl-7-[[4-(1-methylethyl)phenyl]methyl]-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine Dihydroc

Solubility (25°C):

 

体外:

 

DMSO

 

Ethanol

 

Water

 

体内(现配现用):

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

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。

 

生物活性

产品描述

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 70nM,Ki 为 35nM。

靶点

Protease-Activated Receptor (PAR)

Apoptosis

 

体外研究

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.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 75nM,81nM 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.

体内研究

SCH79797 (2.5-250μg/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 25μg/kg.

Animal Model:

Male Sprague Dawley rats (8 weeks of age) with myocardial I/R injury.

Dosage:

2.5μg/kg,10μg/kg,25μg/kg,50μg/kg,100μg/kg,and 250μg/kg

Administration:

Intravenous injection

Result:

Immediately before or during ischemia reduced myocardial necrosis following I/R in the intact rat heart.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

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稀释公式

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  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):