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..

For research use only. We do not sell to patients.

FR-171113 Chemical Structure

FR-171113 Chemical Structure

CAS No. : 173904-50-2

Size Price Stock Quantity
5 mg USD 423 Get quote 2 weeks 1 week
10 mg USD 677 Get quote 2 weeks 1 week
50 mg   Get quote  
100 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

FR-171113 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

FR-171113 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
FR-171113
Cat. No.:
HY-108555
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.