TFLLR-NH2 |
| Catalog No.GC17444 |
TFLLR-NH2는 EC50이 1.9μM인 선택적 PAR1 작용제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 197794-83-5
Sample solution is provided at 25 µL, 10mM.
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TFLLR-NH2 is a selective PAR1 agonist with an EC50 of 1.9 μM.
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].
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].
References:
[1]. de Garavilla L, et al. Agonists of proteinase-activated receptor 1 induce plasma extravasation by a neurogenic mechanism. Br J Pharmacol. 2001 Aug;133(7):975-87.
[2]. Kawabata A, et al. Characterization of the protease-activated receptor-1-mediated contraction and relaxation in the rat duodenal smooth muscle.
[3]. Jia Y, et al. Activation of platelet protease-activated receptor-1 induces epithelial-mesenchymal transition and chemotaxis of colon cancer cell line SW620. Oncol Rep. 2015 Jun;33(6):2681-8.
Animal experiment: | Mice: 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 (33.3mg/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: [1]. de Garavilla L, et al. Agonists of proteinase-activated receptor 1 induce plasma extravasation by a neurogenic mechanism. Br J Pharmacol. 2001 Aug;133(7):975-87. | |
| Cas No. | 197794-83-5 | SDF | |
| Chemical Name | (S,Z)-2-((Z)-((S)-2-((Z)-((2S,3R)-2-amino-1,3-dihydroxybutylidene)amino)-1-hydroxy-3-phenylpropylidene)amino)-N-((S,Z)-1-(((S)-5-guanidino-1-hydroxy-1-iminopentan-2-yl)imino)-1-hydroxy-4-methylpentan-2-yl)-4-methylpentanimidic acid | ||
| Canonical SMILES | CC(C[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])[C@@](O)([H])C)([H])CC1=CC=CC=C1)([H])CC(C)C)([H])/C(O)=N/[C@@](C(O)=N)([H])CCCNC(N)=N)C | ||
| Formula | C31H53N9O6 | M.Wt | 647.82 |
| Solubility | Soluble to 1 mg/ml in 20% acetonitrile / sterile water | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5436 mL | 7.7182 mL | 15.4364 mL |
| 5 mM | 0.3087 mL | 1.5436 mL | 3.0873 mL |
| 10 mM | 0.1544 mL | 0.7718 mL | 1.5436 mL |
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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