TFLLR-NH2 (TFA) is a selective PAR1 agonist with an EC50 of 1.9 μM. It stimulates concentration-dependent increases in [Ca2+]i, upregulates E-cadherin, and downregulates vimentin expression in SW620 cells. It also induces a dose-dependent increase of secreted TGF-β1 in activated platelets. In vivo, it causes marked and sustained oedema and Evans blue extravasation, and produces contraction and relaxation in rat duodenal smooth muscle.
- Selective PAR1 agonist with an EC50 of 1.9 μM
- Appears as a white to off-white solid
- Soluble in DMSO and H2O at 100 mg/mL
- Upregulates E-cadherin and downregulates vimentin expression
- Induces dose-dependent increase of secreted TGF-β1
- Stimulates oedema and Evans blue extravasation in vivo
- Produces contraction and relaxation in rat duodenal smooth muscle