TFLLR-NH2(TFA) 产品活性：TFLLR-NH2 (TFA) 是选择性的 PAR1 激动剂，EC50 值为 1.9 μM。 产品来源： https://www.medchemexpress.cn/TFLLR-NH2_TFA_.html 研究领域：GPCR/G Protein 作用靶点：Protease Activated Receptor (PAR) In Vitro: PAR1 agonists stimulate concentration-dependent increases in [Ca2+]i and in the proportions of neurones. The maximal increase in [Ca2+]i above basal is detected in response to 10 μm TF-NH2 (peak 196.5±20.4 nM, n=25) when 50–80% of identified neurones responded. SW620 cells cultured in the supernatant of TFLLR-NH2-activated platelets upregulate E-cadherin expression and downregulate the vimentin expression. In the in vitro platelet culture system, a TFLLR-NH2 dose-dependent increase of secreted TGF-β1 is detected in the supernatant. In Vivo: Injection of TF-NH2 into the rat paw stimulates a marked and sustained oedema. An NK1R antagonist and ablation of sensory nerves with capsaicin inhibit oedema by 44% at 1 h and completely by 5 h. In wild-type but not PAR1−/− mice, TF-NH2 stimulates Evans blue extravasation in the bladder, oesophagus, stomach, intestine and pancreas by 2–8 fold. Extravasation in the bladder, oesophagus and stomach is abolished by an NK1R antagonist. TFp-NH2 produces notable contraction at 3-50 μM and relaxation at 0.3-50 μM, in the absence of apamin. The concentration-response curve for TFp-NH2-induced contraction is remarkably shifted left, when the TFp-NH2-induced relaxation is blocked by apamin at 0.1 μM. 相关产品：Bioactive Compound Library Plus | Peptide Library | Vorapaxar | TRAP-6 | Trypsin | AZ3451 | SLIGRL-NH2 | PAR-4 Agonist Peptide, amide TFA | 2-Furoyl-LIGRLO-amide | SCH79797 | GB-88 | Protease-Activated Receptor-2, amide | BMS-986120 | GB-110 hydrochloride | AZ8838 | I-191 | AC-55541 | FSLLRY-NH2 TFA | Parmodulin 2 | ENMD-1068 hydrochloride | PZ-128 | Atopaxar | PAR-4 Agonist Peptide, amide | PAR-2-IN-1 | Protease-Activated Receptor-4 | PAR-2 (1-6) (human) | tcY-NH2 TFA | VKGILS-NH2 | Protease-Activated Receptor-1, PAR-1 Agonist TFA 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。