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FR-171113

CAS No. : 173904-50-2

MCE 站：FR-171113

产品活性：FR171113 是一种特异性的非肽类凝血酶受体 (thrombin receptor) 拮抗剂。FR171113 是 PAR1 拮抗剂，具有抗血栓形成作用。 FR171113 抑制凝血酶诱导的血小板聚集，IC₅₀ 为 0.29 μM。

研究领域：GPCR/G Protein

作用靶点：Protease-Activated Receptor (PAR)

In Vitro: FR171113 shows antiplatelet effect on the aggregation of guinea pig platelets induced by PAR1 agonist peptide and thrombin in vitro with IC₅₀s of 1.5 and 0.35 μM, respectively.
FR171113 (0.032-1 μM) dose-dependently inhibits platelet aggregation induced by both thrombin and TRAP-6.
FR171113 significantly prevents the plasma-elicited up-regulation of RAGE, MCP-1 and ICAM-1 mRNA levels in HUVECs.
FR171113 (1 μM; pretreatment for 30 minutes) inhibits thrombin- and SFLLRN (human PAR1 agonist peptide)-induced ERK activation, but not factor Xa- or SLIGKV (PAR2 agonist peptide)-induced ERK activation, indicating that activation of ERK by factor Xa is specifically mediated by PAR2 in mesangial cells.

In Vivo: FR171113 suppresses occlusive thrombosis dose dependently and causes significant prolongation at 1 mg/kg s.c. in the carotid artery thrombosis model.FR171113 shows antiplatelet and antithrombotic effects in vivo. FR171113 is a useful agent for investigating antithrombotic actions via PAR1 in vivo.

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