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编 号：F208693
分子式：C19H11Cl3N2O4S
分子量：469.73
分子式：C19H11Cl3N2O4S
分子量：469.73
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CAS No: 173904-50-2
产品详情
生物活性：
FR171113 is a specific and non-peptide thrombin receptor antagonist. FR171113 exhibits the antithrombotic effects of a PAR1 antagonist. FR171113 inhibits thrombin-induced platelet aggregation with an IC50 of 0.29 μM..
体内研究：
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.Animal Model:Male Hartley guinea pigs (650–950 g) were anesthetized with urethane (1.25 g/kg, i.p.)
Dosage:0.32, 1.0, and 3.2 mg/kg
Administration:Administered subcutaneously (s.c.)
Result:Pretreatment with FR171113 prolonged this parameter in a dose-dependent manner. The time to thrombotic occlusion for 0.32, 1.0 and 3.2 mg/kg of FR171113 was 30.7±5.36, 44.7±8.41 and 92.6±9.79, respectively.
体外研究：
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.
FR171113 is a specific and non-peptide thrombin receptor antagonist. FR171113 exhibits the antithrombotic effects of a PAR1 antagonist. FR171113 inhibits thrombin-induced platelet aggregation with an IC50 of 0.29 μM..
体内研究：
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.Animal Model:Male Hartley guinea pigs (650–950 g) were anesthetized with urethane (1.25 g/kg, i.p.)
Dosage:0.32, 1.0, and 3.2 mg/kg
Administration:Administered subcutaneously (s.c.)
Result:Pretreatment with FR171113 prolonged this parameter in a dose-dependent manner. The time to thrombotic occlusion for 0.32, 1.0 and 3.2 mg/kg of FR171113 was 30.7±5.36, 44.7±8.41 and 92.6±9.79, respectively.
体外研究：
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.
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