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CAS No. : 1262750-73-1
MCE 国际站:tcY-NH2 TFA
产品活性:tcY-NH2 ((trans-Cinnamoyl)-YPGKF-NH2) TFA 是一种有效的 PAR4 选择性肽类拮抗剂。tcY-NH2 TFA 抑制凝血酶和 AY-NH2 诱导的血小板聚集和内皮抑素释放,可用于炎症、免疫学的研究。
研究领域:GPCR/G Protein
作用靶点:Protease Activated Receptor (PAR)
In Vitro: tcY-NH2 TFA (0-500 μM) inhibits AYPGKF-NH2 (10 μM)-induced platelet (obtained from male albino Sprague–Dawley rats) aggregation, with an IC50 value of 95 μM.
tcY-NH2 TFA potently activates aorta relaxation (RA) and gastric (LM) contraction, with IC50 values of 64 μM (RA) and 1 μM (LM).
tcY-NH2 TFA (Tc-YPGKF-NH2, 400 μM, 5 min) prevents endostatin release and platelet aggregation induced by thrombin or by AY-NH2.
tcY-NH2 TFA (5 μM, 15 min) decreases infarct size (IS) by 51%, and increases recovery of ventricular function by 26% in an isolated heart model.
In Vivo: tcY-NH2 TFA (tail vein injection, 0.6 mg/kg for a single dose) alleviates liver injury in Brain death (BD) rat model, indicated by lower serum ALT/AST levels and better histomorphology.
tcY-NH2 TFA (intraperitoneal injection, 0.6 mg/kg for a single dose) increases posttraumatic activation of CD4+ Tregs within the draining lymph nodes in burn injury mice model .
tcY-NH2 TFA (intrapleural injection, 40 ng/kg for a single dose) inhibits neutrophil recruitment in experimental inflammation in mice.
相关产品:Covalent Screening Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Covalent Screening Library | Targeted Diversity Library | Peptide Library | Coagulation and Anti-coagulation Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Protease-Activated Receptor-3 (PAR-3) (1-6), human | I-191 | FSLLRY-NH2 TFA | VKGILS-NH2 | AC-55541 | FR-171113 | Protease-Activated Receptor-1 antagonist 3 | PAR-4 Agonist Peptide, amide TFA | Aeruginosin 98-B | AZ3451 | 2-Furoyl-LIGRLO-amide | AC-264613 | tcY-NH2 | ENMD-1068 hydrochloride | SLIGRL-NH2 | Protease-Activated Receptor-1, PAR-1 Agonist | CBK289001 | GB-110 hydrochloride | PAR-4 Agonist Peptide, amide | GB-88 | RWJ-56110 | Trypsin (MS grade) | AZ8838 | TRAP-6 | UDM-001651 | Parmodulin 2 | TFLLR-NH2 | Vorapaxar | SCH79797 dihydrochloride | TRAP-6-IN-1
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