计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,避光,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC 50 =0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 ( IC 50 =0.16 μM) and thrombin ( IC 50 =0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis
In Vitro
Proteinase-activated receptors (PARs) are a family of G protein-coupled receptors activated by the proteolytic cleavage of their N-terminal extracellular domain, exposing a new amino terminal sequence that functions as a tethered ligand to activate the receptors. RWJ56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC 50 =0.16 μM) and thrombin (IC 50 =0.34 μM) while being quite selective relative to collagen and the thromboxane mimetic U46619 . RWJ-56110 dihydrochloride is fully inhibits thrombin-induced RASMC proliferation with an IC 50 value of 3.5 μM. RWJ-56110 dihydrochloride shows blockade of thrombin’s action with RASMC calcium mobilization (IC 50 =0.12 μM), as well as with HMVEC (IC 50 =0.13 μM) and HASMC calcium mobilization (IC 50 =0.17 μM). RWJ56110 (0.1-10 μM; 24-96 hours) inhibits endothelial cell growth dose-dependently, with half-maximal inhibitory concentration of RWJ56110 is approximately 10 μM. RWJ56110 (0.1-10 μM; 6 hours) inhibits DNA synthesis of endothelial cells in a thymidine incorporation assays. Endothelial cells are in fast-growing state (50-60% confluence), RWJ56110 inhibits cell DNA synthesis in a dose-dependent manner, but when cells that are in the quiescent state (100% confluent), the inhibitory effect of PAR-1 antagonists is much less pronounced. RWJ56110 (0.1-10 μM; pretreatment for 15 min) inhibits thrombin-induced Erk1/2 activation in a concentration-dependent manner. However, when endothelial cells are stimulated by FBS (final concentration 4%), it reduces partially the activated levels of Erk1/2. RWJ56110 (30 μM; 24 hours) has an inhibitory effect on endothelial cell cycle progression. It reduces the percentage of cells in the S phase, while alterations in the percentages of G1 and G2/M cells are less pronounced. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Endothelial cells Concentration: 0 μM; 3 μM; 1 μM; 3 μM; 10 μM Incubation Time: Pretreatment for 15 min Result: Resulted in MAPK activation in Endothelial cells. Cell Cycle AnalysisCell Line: Endothelial cells Concentration: 0 μM; 3 μM; 1 μM; 3 μM; 10 μM Incubation Time: Pretreatment for 15 min Result: Reduced cell number in S phase.
Form:Solid
IC50& Target:IC50: 0.44 uM (PAR-1) IC50: 0.16 μM (the aggregation of human platelets induced by SFLLRN-NH2) IC50: 0.34 μM (the aggregation of human platelets induced by thrombin)
规格
别名
RWJ-56110 二盐酸盐
规格或纯度
≥99%
英文名称
RWJ-56110 dihydrochloride
生化机理
RWJ-56110 二盐酸盐是 PAR-1 活化和内化的强效、选择性、多肽模拟抑制剂（结合 IC 50 =0.44 uM），对 PAR-2、PAR-3 或 PAR-4 没有影响。RWJ-56110 二盐酸盐可抑制人血小板的聚集。
储存条件
2-8°C储存,避光,干燥
运输条件
低温运输
纯度
≥99%
名称和识别符
分子类型
小分子
Smiles
O=C(N[C@H](C(NCC1=CC=CC=C1)=O)CCN)[C@@H](NC(NC2=CC3=C(C=C2)C(CN4CCCC4)=CN3CC5=C(Cl)C=CC=C5Cl)=O)CC6=CC=C(F)C(F)=C6.[H]Cl.[H]Cl
分子量
863.65
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 200 mg/mL (231.58 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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