TFLLR-NH2 (TFA) is a selective PAR1 agonist with an EC50 of 1.9 μM.
CAT No: 10-101-204
CAS No:1313730-19-6
Synonyms/Alias:TFLLR-NH2(TFA);TFLLR-NH2 TFA;1313730-19-6;(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;2,2,2-trifluoroacetic acid;HY-P0226A;DA-78364;MS-31362;CS-0058948;G13320;TFLLR-NH2 TFA, TFLLR-NH2 trifluoroacetate salt;TFLLR-NH2 trifluoroacetate salt, >98% (HPLC);(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; TRIFLUOROACETIC ACID;(S)-2-((S)-2-((2S,3R)-2-Amino-3-hydroxybutanamido)-3-phenylpropanamido)-N-((S)-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)-4-methylpentanamide 2,2,2-trifluoroacetate;
TFLLR-NH2(TFA), also known as the thrombin receptor-activating peptide or PAR-1 agonist peptide, is a synthetic pentapeptide widely recognized for its utility in studying protease-activated receptor-1 (PAR-1) signaling. Structurally derived from the tethered ligand sequence of the human thrombin receptor, TFLLR-NH2(TFA) mimics the endogenous activation motif, enabling precise experimental modulation of PAR-1 activity in diverse biological systems. Its high specificity and stability make it a valuable biochemical tool for dissecting G-protein-coupled receptor (GPCR) pathways, platelet function, and cellular responses to proteolytic stimuli. The compound's trifluoroacetate (TFA) salt form further enhances its solubility and handling in laboratory settings, supporting a broad range of peptide-based research applications.
Receptor Activation Studies: As a potent and selective PAR-1 agonist, TFLLR-NH2(TFA) is extensively employed to investigate thrombin receptor signaling mechanisms in vitro. Researchers utilize this peptide to activate PAR-1 independently of thrombin, enabling the dissection of downstream signaling cascades such as calcium mobilization, MAPK pathway activation, and cytoskeletal rearrangements. This approach circumvents the pleiotropic effects of thrombin, allowing for more precise attribution of observed cellular responses to PAR-1 engagement.
Platelet Function Assays: The peptide serves as a reliable tool for probing platelet activation and aggregation processes mediated by PAR-1. By mimicking thrombin's action on platelets, TFLLR-NH2(TFA) facilitates the study of intracellular signaling events, granule secretion, integrin activation, and platelet-leukocyte interactions under controlled experimental conditions. Its use in flow cytometry, aggregometry, and fluorescence-based assays provides insights into the molecular basis of hemostasis and thrombosis, supporting both basic and translational research in vascular biology.
Signal Transduction Research: TFLLR-NH2(TFA) is instrumental in elucidating the broader roles of GPCR-mediated signaling beyond hemostatic systems. Researchers employ this peptide in various cell types, including endothelial cells, smooth muscle cells, and fibroblasts, to examine PAR-1-dependent pathways involved in cell proliferation, migration, and inflammation. Its application enables the identification of novel signaling intermediates and cross-talk with other receptor systems, contributing to a deeper understanding of cellular communication networks.
Pharmacological Screening: In drug discovery and pharmacological profiling, TFLLR-NH2(TFA) is utilized as a reference agonist for screening PAR-1 antagonists and modulators. The peptide's consistent activity and receptor specificity make it suitable for high-throughput screening platforms, where it assists in evaluating the efficacy, selectivity, and mechanism of action of candidate compounds targeting the thrombin receptor. This facilitates the development of new molecular probes and potential therapeutic agents for disorders involving aberrant PAR-1 signaling.
Peptide Structure-Function Analysis: The defined sequence and functional properties of TFLLR-NH2(TFA) make it an excellent model for structure-activity relationship (SAR) studies within the context of peptide-GPCR interactions. Researchers can employ this compound as a template for designing and testing analogs with modified amino acid residues, altered receptor selectivity, or enhanced stability. Such investigations advance the rational design of novel peptide ligands and contribute to the broader field of peptide-based drug discovery and receptor biology.
3. Adipose tissue is a key organ for the beneficial effects of GLP-2 metabolic function
5. Autoinhibition and phosphorylation-induced activation of phospholipase C-γ isozymes
If you have any peptide synthesis requirement in mind, please do not hesitate to contact us at . We will endeavor to provide highly satisfying products and services.
Creative Peptides is a trusted CDMO partner specializing in high-quality peptide synthesis, conjugation, and manufacturing under strict cGMP compliance. With advanced technology platforms and a team of experienced scientists, we deliver tailored peptide solutions to support drug discovery, clinical development, and cosmetic innovation worldwide.
From custom peptide synthesis to complex peptide-drug conjugates, we provide flexible, end-to-end services designed to accelerate timelines and ensure regulatory excellence. Our commitment to quality, reliability, and innovation has made us a preferred partner across the pharmaceutical, biotechnology, and personal care industries.
Read More