TFLLR-NH2 is a selective PAR1 agonist with an EC50 of 1.9 μM.
CAT No: R1713
CAS No:197794-83-5
Synonyms/Alias:TFLLR-NH2;197794-83-5;Thr-Phe-Leu-Leu-Arg-amide;(2S)-N-[(2S)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanamide;H-Thr-Phe-Leu-Leu-Arg-NH2;PAR1-AP;GTPL3742;CHEMBL4065100;L-Argininamide, L-threonyl-L-phenylalanyl-L-leucyl-L-leucyl-;HY-P0226;HB2921;AKOS024456615;CS-6494;TFLLR (modifications: C-terminal amide);AC-32571;AS-76215;DA-48902;FT109632;PEPTIDE1{T.F.L.L.R.[am]}$$$$;(Thr1)-PAR-1 (1-5) amide (human) trifluoroacetate salt;l-threonyl-l-phenylalanyl-l-leucyl-l-leucyl-l-argininamide;(2S)-2-[(2S)-2-[(2S,3R)-2-amino-3-hydroxybutanamido]-3-phenylpropanamido]-N-[(1S)-1-{[(1S)-4-carbamimidamido-1-carbamoylbutyl]carbamoyl}-3-methylbutyl]-4-methylpentanamide;TFLLRamide, (Thr(1))-TRAP-5 amide, TFLLR-NH2 Protease-Activated Receptor 1 (PAR1) Agonist;(Thr1)-PAR-1 (1-5) amide (human);
TFLLR-NH2 is a synthetic peptide that serves as a selective agonist for protease-activated receptor-1 (PAR-1), a member of the G-protein-coupled receptor family involved in various cellular signaling pathways. Structurally, it mimics a segment of the tethered ligand domain exposed upon thrombin cleavage of PAR-1, enabling researchers to activate the receptor independently of proteolytic activity. The peptide's defined sequence and amide-modified C-terminus confer stability and receptor specificity, making it a valuable tool for dissecting PAR-1-mediated mechanisms in cellular and molecular studies. Its utility spans signal transduction research, platelet biology, vascular physiology, and the broader exploration of protease-activated receptor functions in health and disease models.
Signal transduction studies: TFLLR-NH2 is widely used to probe the intracellular signaling cascades initiated by PAR-1 activation. By selectively stimulating PAR-1, scientists can delineate downstream pathways such as phospholipase C activation, intracellular calcium mobilization, and MAP kinase signaling. This enables detailed characterization of receptor-specific responses across diverse cell types, including endothelial cells, smooth muscle cells, and platelets, thereby advancing the understanding of G-protein-coupled receptor signaling dynamics.
Platelet activation assays: As a potent PAR-1 agonist, the peptide is employed in platelet function studies to mimic thrombin-induced activation without the confounding effects of proteolysis or secondary mediators. Researchers utilize it to investigate platelet aggregation, secretion, and integrin activation, facilitating the evaluation of antiplatelet agents or the elucidation of distinct signaling events that regulate hemostasis and thrombosis. Its use supports both basic research into platelet biology and the development of novel anti-thrombotic strategies.
Vascular biology research: The ability of TFLLR-NH2 to selectively activate PAR-1 makes it an important reagent in studies of vascular tone regulation, endothelial barrier function, and inflammatory signaling within the vasculature. By applying the peptide to cultured endothelial or smooth muscle cells, investigators can model the effects of thrombin receptor engagement under controlled experimental conditions. Such studies yield insights into mechanisms underlying vascular permeability, leukocyte adhesion, and the interplay between coagulation and inflammation.
Pharmacological screening: The peptide is instrumental in the pharmacological profiling of PAR-1-targeted compounds. It serves as a reference agonist in assays designed to characterize the potency and selectivity of novel antagonists or modulators. By providing a consistent and specific means of receptor activation, TFLLR-NH2 enables robust comparative studies that inform drug discovery efforts targeting thrombin receptor signaling pathways.
Receptor desensitization and trafficking studies: In cellular models, repeated or sustained exposure to TFLLR-NH2 allows researchers to investigate the processes of PAR-1 desensitization, internalization, and recycling. This application is critical for understanding how receptor responsiveness is regulated in physiological and pathological contexts. By quantifying changes in receptor surface expression and downstream signaling following peptide stimulation, scientists can elucidate adaptive mechanisms that modulate cellular sensitivity to protease-activated receptor ligands.
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