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Protease-activated receptor 1 (PAR1) antagonist. Exhibits potent antiplatelet activity in vitro; inhibits thrombin TRAP-6-induced platelet aggregation (IC50 = 2.5 μM) with no effect on coagulation time.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 469.73. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.1 mM||21.29 mL||106.44 mL||212.89 mL|
|0.5 mM||4.26 mL||21.29 mL||42.58 mL|
|1 mM||2.13 mL||10.64 mL||21.29 mL|
|5 mM||0.43 mL||2.13 mL||4.26 mL|
References are publications that support the biological activity of the product.
Kato et al (1999) In vitro antiplatelet profile of FR171113, a novel non-peptide thrombin receptor antagonist. Eur.J.Pharmacol. 384 197 PMID: 10611442
Kato et al (2003) Inhibition of arterial thrombosis by a protease-activated receptor 1 antagonist, FR171113, in the guinea pig. Eur.J.Pharmacol. 473 163 PMID: 12892834
If you know of a relevant reference for FR 171113, please let us know.
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Keywords: FR 171113, FR 171113 supplier, FR171113, thrombin, protease-activated, receptor, 1, PAR1, antagonist, antagonists, antithrombotic, antiplatelet, Protease-Activated, Receptors, 3643, Tocris Bioscience
1 Citation for FR 171113
Citations are publications that use Tocris products. Selected citations for FR 171113 include:
Eum et al (2014) Disruption of epithelial barrier by quorum-sensing N-3-(oxododecanoyl)-homoserine lactone is mediated by matrix metalloproteinases. Am J Physiol Gastrointest Liver Physiol 306 G992 PMID: 24742991
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Reviews for FR 171113
Average Rating: 3 (Based on 1 Review.)
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To attempt to block TRAP6 mediated Ca2+ mobilization in human pericytes. Its lack of potency and low solubility means it was not especially effective even with sub-maximal agonist concentrations - some antagonism or slowing of response - but not the complete block I had hoped for even when pre-equilibrated prior to agonist activation. We will now save our pennies to try the more potent SCH PAR1 antag
Really could not get this to dissolve at 10 mM in DMSO as website suggests - probably goes in around 7 mM. As this is not a very potent antagonist you will need to have quite a bit of DMSO around to get even partial antagonism.
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