1. GPCR/G Protein
  2. Protease-Activated Receptor (PAR)
  3. FR-171113

FR-171113 

Cat. No.: HY-108555
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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..

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FR-171113 Chemical Structure

FR-171113 Chemical Structure

CAS No. : 173904-50-2

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Description

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.[1][2][3][4].

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[2].
FR171113 (0.032-1 μM) dose-dependently inhibits platelet aggregation induced by both thrombin and TRAP-6[1].
FR171113 significantly prevents the plasma-elicited up-regulation of RAGE, MCP-1 and ICAM-1 mRNA levels in HUVECs[2].
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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Human washed platelets
Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time:
Result: The IC50 value for thrombin-induced platelet aggregation was 0.29 μM. The IC50 value for TRAP-6-induced platelet aggregation was 0.15 μM.

RT-PCR[2]

Cell Line: human umbilical vein endothelial cells (HUVECs)
Concentration: 1 μM
Incubation Time: 4 hours
Result: 3% citrated human plasma-evoked ROS generation, RAGE, MCP-1 and ICAM-1 gene induction was significantly blocked.

Western Blot Analysis[3]

Cell Line: Mesangial cells
Concentration: 1 μM
Incubation Time: Pretreatment for 30 minutes
Result: Pretreatment inhibited thrombin (10 nM; for 5 minutes)- and SFLLRN(100 μM for 5 minutes)-induced ERK activation.
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[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Hartley guinea pigs (650–950 g) were anesthetized with urethane (1.25 g/kg, i.p.)[4]
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.
Molecular Weight

469.73

Formula

C₁₉H₁₁Cl₃N₂O₄S

CAS No.
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FR-171113
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HY-108555
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