1313730-19-6
1313730-19-6 structure
- Name: TFLLR-NH2 TFA
- Chemical Name: TFLLR-NH2(TFA)
- CAS Number: 1313730-19-6
- Molecular Formula: C33H54F3N9O8
- Molecular Weight: 761.83
- Catalog: Peptides
- Create Date: 2018-11-18 07:56:02
- Modify Date: 2025-08-23 12:11:20
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TFLLR-NH2 (TFA) is a selective PAR1 agonist with an EC50 of 1.9 μM.
| Name | TFLLR-NH2(TFA) |
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| Synonyms | MFCD05663482 |
| Description | TFLLR-NH2 (TFA) is a selective PAR1 agonist with an EC50 of 1.9 μM. |
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| Related Catalog | |
| Target |
EC50: 1.9 μM (PAR1)[1] |
| 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[1]. 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[2]. |
| 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[1]. 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[3]. |
| Animal Admin | Mice[1] Mice are anaesthetized with isofluorane, and saline or TF-NH2 (3 μmol/kg in 25 μL physiological saline) is injected into the lateral tail vein. Evans blue (33.3 mg/kg in 50 μL saline) is co-injected with the peptide. Mice are perfused transcardially at 10 min after administration of TF-NH2 with physiological saline containing 20 u/mL heparin at a pressure of 80-100 mmHg for 2-3 min. Excised tissues are incubated in 1 mL of formamide for 48 h, and Evans blue content is measured spectrophotometrically at 650 nm[1]. |
| References |
| Molecular Formula | C33H54F3N9O8 |
|---|---|
| Molecular Weight | 761.83 |
| Hazard Codes | Xi |
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