1313730-19-6

中文名称:

1313730-19-6

中文同义词:

英文名称:

TFLLR-NH2(TFA)

英文同义词:

TFLLR-NH2(TFA);197794-83-5 (Thr1)-TRAP-5 amide

CAS号:

1313730-19-6

分子式:

C33H54F3N9O8

分子量:

761.85

EINECS号:

相关类别:

多肽;多肽

Mol文件:

1313730-19-6.mol

生物活性

TFLLR-NH2 (TFA) 是选择性的 PAR1 激动剂，EC50 值为 1.9 μM。

靶点

EC50: 1.9 μM (PAR1)

体外研究

PAR1 agonists stimulate concentration-dependent increases in [Ca 2+ ]i and in the proportions of neurones. The maximal increase in [Ca 2+ ]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.

体内研究

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.