Protease-Activated Receptor-1, PAR-1 Agonist TFA is a selective protease-activated receptor 1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist TFA corresponds to the PAR1 ligand and can selectively mimic the action of thrombin through this receptor.

Physicochemical Properties

Molecular Formula	C37H59F3N10O11
Molecular Weight	876.92
Related CAS #	Protease-Activated Receptor-1, PAR-1 Agonist;141136-85-8
Appearance	White to off-white solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro

In human HT-29 colon cancer cells that express PAR1 endogenously, protease-activated receptor-1, PAR-1 antagonist, activates protein kinase C isoenzymes alpha and epsilon. At the cellular level, HT-29 cell migration and matrix adhesion were induced by Protease-Activated Receptor-1, PAR-1 Agonist, and thrombin through a PKCepsilon-dependent mechanism. This was determined by the fact that the PKC inhibitors bisindolylmaleimide I and the PKCepsilon translocation inhibitory peptide EAVSLKPT, but not Gö 6976, inhibited the effects of PAR1-mediated processes.

References

[1]. Thrombin-induced ATP release from human umbilical vein endothelial cells. Am J Physiol Cell Physiol. 2012 Mar 15;302(6):C915-23. [2]. PAR1-type thrombin receptor stimulates migration and matrix adhesion of human colon carcinoma cells by a PKCepsilon-dependent mechanism. Oncol Res. 2004;14(10):475-482.

Solubility Data

Solubility (In Vitro)	H2O :~6.67 mg/mL (~7.61 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 5 mg/mL (5.70 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.1404 mL	5.7018 mL	11.4035 mL
	5 mM	0.2281 mL	1.1404 mL	2.2807 mL
	10 mM	0.1140 mL	0.5702 mL	1.1404 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.