化合物TFLLR-NH2(2TFA)
TFLLR-NH2(L-Threonyl-L-Phenylalanyl-L-Leucyl-L-Leucyl-L-Argininamide)
CAS: 197794-83-5
化学式: C31H53N9O6
| 中文名 | TFLLR-NH2 |
| 英文名 | L-Threonyl-L-Phenylalanyl-L-Leucyl-L-Leucyl-L-Argininamide |
| 别名 | 血酶受体 化合物TFLLR-NH2(2TFA) |
| 英文别名 | TFLLR-NH2 TFLLR-AMIDE (Thr1)-TRAP-5 amide THR-PHE-LEU-LEU-ARG-NH2 H-THR-PHE-LEU-LEU-ARG-NH2 THROMBIN RECEPTOR (PAR-1), HYBRIDE HUMAN-XENOPE TFLLR-NH2 Protease-Activated Receptor 1 (PAR1) Agonist L-Threonyl-L-Phenylalanyl-L-Leucyl-L-Leucyl-L-Argininamide (2S)-N-[(2S)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanamide |
| CAS | 197794-83-5 |
| 化学式 | C31H53N9O6 |
| 分子量 | 647.81 |
| 密度 | 1.31±0.1 g/cm3(Predicted) |
| 酸度系数 | 12.10±0.45(Predicted) |
| 存储条件 | -20℃ |
| 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. |
化合物TFLLR-NH2(2TFA) - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.544 ml | 7.718 ml | 15.437 ml |
| 5 mM | 0.309 ml | 1.544 ml | 3.087 ml |
| 10 mM | 0.154 ml | 0.772 ml | 1.544 ml |
| 5 mM | 0.031 ml | 0.154 ml | 0.309 ml |
最后更新：2024-01-02 23:10:35
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