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TFLLR-NH2(TFA)

CAS No. : 1313730-19-6

MCE 站：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。

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  |  TRAP-6  |  AZ3451  |  PAR-4 Agonist Peptide, amide TFA  |  SCH79797 dihydrochloride  |  Protease-Activated Receptor-2, amide  |  ENMD-1068 hydrochloride  |  SLIGRL-NH2  |  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  |  TFLLR-NH2  |  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

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