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RWJ-56110

CAS No. : 252889-88-6

MCE 站：RWJ-56110

产品活性：RWJ-56110 是一种有效的、选择性的、拟肽抑制剂，抑制 PAR-1 激活和内化 (结合 IC₅₀=0.44 uM)，对PAR-2, PAR-3 和 PAR-4 无影响。RWJ-56110 抑制由 SFLLRN-NH2?(IC₅₀=0.16 μM) 和凝血酶(IC₅₀=0.34 μM) 诱导的血小板聚集，相对于 U46619 (HY-108566) 具有相当的选择性。RWJ-56110 在体内阻断血管生成和新血管的形成。RWJ-56110 诱导细胞凋亡 (apoptosis)。

研究领域：GPCR/G Protein  |  Apoptosis

作用靶点：Protease-Activated Receptor (PAR)  |  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?(IC₅₀=0.16 μM) and thrombin (IC₅₀=0.34 μM) while being?quite selective?relative to collagen and the thromboxane mimetic U46619 (HY-108566).
RWJ-56110 is fully inhibits thrombin-induced RASMC proliferation with an IC₅₀ value of 3.5 μM. RWJ-56110 shows blockade of thrombin’s action with RASMC calcium mobilization (IC₅₀=0.12 μM), as well as with HMVEC (IC₅₀=0.13 μM) and HASMC calcium mobilization (IC₅₀=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.

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