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1313730-19-6

中文名稱(chēng) 1313730-19-6
英文名稱(chēng) TFLLR-NH2(TFA)
CAS 1313730-19-6
分子式 C33H54F3N9O8
分子量 761.85
MOL 文件 1313730-19-6.mol
更新日期 2024/12/23 10:30:27
1313730-19-6 結(jié)構(gòu)式 1313730-19-6 結(jié)構(gòu)式

基本信息

中文別名
激動(dòng)劑TFLLR-NH2
(S)-2-((S)-2-((2S,3R)-2-氨基-3-羥基丁酰胺基)-3-苯基丙酰胺基)-N-((S)-1-((S)-1-氨基-5-胍基-1-氧代戊-2-基)氨基)-4-甲基-1-氧代戊-2-基)-4-甲基戊酰胺 2,2,2-三氟乙酸鹽
英文別名
TFLLR-NH2(TFA)
197794-83-5 (Thr1)-TRAP-5 amide

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度Water: 100 mg/mL (131.26 mM); DMSO: 100 mg/mL (131.26 mM)
形態(tài)Solid
顏色White to off-white
序列H-Thr-Phe-Leu-Leu-Arg-NH2

常見(jiàn)問(wèn)題列表

生物活性
TFLLR-NH2 (TFA) 是選擇性的 PAR1 激動(dòng)劑,EC50 值為 1.9 μM。
靶點(diǎn)

EC50: 1.9 μM (PAR1)

體外研究

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.

體內(nèi)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.

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