MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

TFLLR-NH2

CAS No. : 197794-83-5

MCE 站：TFLLR-NH2

产品活性：TFLLR-NH2是选择性的PAR1激动剂，EC₅₀值为1.9 μM。

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：TRAP-6  |  AZ3451  |  PAR-4 Agonist Peptide, amide TFA  |  SCH79797 dihydrochloride  |  Protease-Activated Receptor-2, amide  |  ENMD-1068 hydrochloride  |  SLIGRL-NH2  |  TFLLR-NH2(TFA)  |  GB-110 hydrochloride  |  2-Furoyl-LIGRLO-amide  |  AC-55541  |  FSLLRY-NH2 TFA  |  Protease-Activated Receptor-4  |  Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA  |  tcY-NH2 TFA  |  AC-264613  |  Atopaxar  |  PAR 4 (1-6) (TFA)  |  Parstatin(human)  |  Parstatin(mouse)  |  Protease-Activated Receptor-1, PAR-1 Agonist  |  RWJ-56110 dihydrochloride  |  tcY-NH2  |  TRAP-6 amide

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*新*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 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*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。