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

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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Based on 1 publication(s) in Google Scholar

FR-171113 Related Antibodies

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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].

IC50 & Target

PAR1

.29 μM (IC50)

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].

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

FR-171113 Related Antibodies

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].

MedChemExpress (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.
SMILES

O=C(OC)/C=C(S/C(N1C2=CC=C(Cl)C=C2)=N\C(C3=CC=C(Cl)C=C3Cl)=O)/C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FR-171113 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FR-171113173904-50-2FR171113FR 171113Protease Activated Receptor (PAR)Thrombin receptorsThrombinantithromboticPAR1plateletaggregationAntiplateletInhibitorinhibitorinhibit

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