TFLLR-NH2-TFA _Protease-Activated Receptor (PAR) Agonist - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETFLLR-NH2(TFA)Cat. No.: HY-P0226ACAS No.: 1313730-19-6分式: CHFNO分量: 761.83Sequence: Thr-Phe-Leu-Leu-Arg-NH2Sequence Shortening: TFLLR-NH2作靶点: Protease-Activated Receptor (PAR)作通路: GPCR/G Protein储存式: Powder -80C 2 years-20C 1 year

2、In solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (131.26 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.3126 mL 6.5631 mL 13.1263 mL5 mM 0.2625 mL 1.3126 mL 2.6253 mL10 mM 0.1313 mL 0.6563 mL 1.3126 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给

3、药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (3.28 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您边的抑制剂

4、师www.MedChemESolubility: 2.5 mg/mL (3.28 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (3.28 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 TFLLR-NH2 (TFA)是选择性的 PAR1 激动剂，EC50 值为 1.9 M。IC50 & Target EC50: 1.9 M (PAR1) 1体外研究 PAR1 agonists stimulate concentration-dependent incr

5、eases in Ca2+i and in the proportions of neurones.The maximal increase in Ca2+i above basal is detected in response to 10m TF-NH2 (peak 196.520.4nM, n=25) when 5080% of identified neurones responded 1. SW620 cells cultured in the supernatant ofTFLLR-NH2-activated platelets upregulate E-cadherin expr

6、ession and downregulate the vimentin expression.In the in vitro platelet culture system, a TFLLR-NH2 dose-dependent increase of secreted TGF-1 isdetected in the supernatant 2.体内研究 Injection of TF-NH2 into the rat paw stimulates a marked and sustained oedema. An NK1R antagonist andablation of sensory

7、 nerves with capsaicin inhibit oedema by 44% at 1h and completely by 5h. In wild-typebut not PAR1/ mice, TF-NH2 stimulates Evans blue extravasation in the bladder, oesophagus, stomach,intestine and pancreas by 28 fold. Extravasation in the bladder, oesophagus and stomach is abolished byan NK1R antag

8、onist 1. TFp-NH2 produces notable contraction at 3-50 M and relaxation at 0.3-50 M, inthe absence of apamin. The concentration-response curve for TFp-NH2-induced contraction is remarkablyshifted left, when the TFp-NH2-induced relaxation is blocked by apamin at 0.1 M 3.PROTOCOLAnimal Mice 1Administra

9、tion 1 Mice are anaesthetized with isofluorane, and saline or TF-NH2 (3mol/kg in 25L physiological saline) isinjected into the lateral tail vein. Evans blue (33.3mg/kg in 50L saline) is co-injected with the peptide. Miceare perfused transcardially at 10min after administration of TF-NH2 with physiol

10、ogical saline containing 20u/mL heparin at a pressure of 80-100mmHg for 2-3min. Excised tissues are incubated in 1mL of formamidefor 48h, and Evans blue content is measured spectrophotometrically at 650nm 1.MCE has not independently confirmed the accuracy of these methods. They are for reference onl

11、y.REFERENCES1. de Garavilla L, et al. Agonists of proteinase-activated receptor 1 induce plasma extravasation by a neurogenic mechanism. Br JPharmacol. 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 smoothmuscle.3. Jia Y, et al. Activation of platelet protease-activated receptor-1 induces epithelial-mesenchymal transition and chemotaxis of colon2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEcancer cell line SW620. Oncol Rep. 2015 Jun;33(6):2681-8.McePdfHeightCaution: Pro