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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEN-Formyl-Met-Leu-PheCat. No.: HY-P0224CAS No.: 59880-97-6Synonyms: fMLP; N-Formyl-MLF分式: CHNOS分量: 437.55Sequence: Formyl-Met-Leu-PheSequence Shortening: Formyl-MLF作靶点: TNF Receptor作通路: Apoptosis储存式: Powder -80C 2 years-20C 1 yea
2、rIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 82.5 mg/mL (188.55 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2855 mL 11.4273 mL 22.8545 mL5 mM 0.4571 mL 2.2855 mL 4.5709 mL10 mM 0.2285 mL 1.1427 mL 2.2855 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
3、储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 N-Formyl-Met-Leu-Phe (fMLP; N-Formyl-MLF)种趋化肽和N-甲酰基肽受体 (FPR) 的特异性配体。报道显N-Formyl-Met-Leu-Ph 可抑制 TNF-alpha 的分泌。1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEIC50 & Target TNF-alpha 1体外研究 Binding of N-Formyl-Met-Leu-Phe to its specific cell surface receptor, N-formy
4、l peptide receptor (FPR),triggers different cascades of biochemical events, eventually leading to cellular activation. FPR is achemoattractant receptor belonging to the G protein-coupled receptor family. N-Formyl-Met-Leu-Phepromotes osteoblastic commitment and suppresses adipogenic commitment under
5、osteoblastic differentiationconditions. N-Formyl-Met-Leu-Phe stimulates osteogenesis is associated with increased expression ofosteogenic markers and mineralization. N-Formyl-Met-Leu-Phe inhibits expression of peroxisomeproliferator-activated receptor-1. N-Formyl-Met-Leu-Phe-stimulated osteogenic di
6、fferentiation is mediatedvia FPR1-phospholipase C/phospholipase D-Ca2+-calmodulin-dependent kinase II-ERK-CREB signalingpathways 1. N-Formyl-Met-Leu-Phe, a bacterial-derived peptide, induced proinflammatory cytokine geneexpression in human peripheral blood monocytes. Bacterial products LPS and N-For
7、myl-Met-Leu-Phesynergistically induce inflammatory response via multiple signaling pathways. TLR4, IKK-IB, and NF-Bsignaling pathways are involved in the synergistic induction of TNF- via p65 nuclear translocation-dependent mechanisms 2.体内研究 N-Formyl-Met-Leu-Phe promotes bone formation in zebrafish
8、and rabbits. Extensive skeletal development isevident at 5 dpf in over 80% of N-Formyl-Met-Leu-Phe-treated zebrafish. Treatment with N-Formyl-Met-Leu-Phe results in increased expression of Runx2. Bone marrow spaces are widely formed, and connectivetissue covering bone is dense, like periosteum, in N
9、-Formyl-Met-Leu-Phe-treated calvaria 1. N-Formyl-Met-Leu-Phe mediate release of calprotectin from PMN in vitro. It induces release of calprotectin from PMN in adose dependent manner. A minimum of 10% of total PMN calprotectin is retained at concentrations of 0.1-10.0 nM of N-Formyl-Met-Leu-Phe 3.PRO
10、TOCOLCell Assay 2 Cells are cotransfected with either a dominant negative form of IB or a dominant negative form of IKKtogether with the NF-B-dependent luciferase reporter plasmid. The plasmid pCMV is used as a control fortransfection efficiency and this is monitored via the expression of -galactosi
11、dase. Cells are transientlytransfected with plasmids using DEAE-dextran. The transfected cells are cultivated for 48 h before a 6-hincubation in medium N-Formyl-Met-Leu-Phe, LPS, or N-Formyl-Met-Leu-Phe/LPS. Luciferase activity isdetermined by using the luciferase assay kit and a Monolight 3010 lumi
12、nometer 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: N-Formyl-Met-Leu-Phe is prepared in sterile PBS. Under the anesthesia, mice are intranasally treatedAdministration 2 with LPS (0.3 mg/kg) or N-Formyl-Met-Leu-Phe (0.5 mg/kg) or N-For
13、myl-Met-Leu-Phe and LPS in 50 L ofsterile PBS (control), BAL is performed by cannulating the trachea with sterilized PBS, and cells from BALfluid are stained with Wright-Giemsa stain after cytocentrifuge. For TNF- protein release, BAL fluid iscollected and secreted TNF- is measured by ELISA as descr
14、ibed above 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Shin MK, et al. N-formyl-methionyl-leucyl-phenylalanine (fMLP) promotes osteoblast differentiation via the N-formyl peptide recept
15、or 1-mediated signaling pathway in human mesenchymal stem cells from bone marrow. J Biol Chem. 2011 May 13;286(19):17133-43.2. Chen LY, et al. Synergistic induction of inflammation by bacterial products lipopolysaccharide and fMLP: an important microbialpathogenic mechanism. J Immunol. 2009 Feb 15;182(4):2518-24.3. Hetland G, et al. Chemotaxins C5a and fMLP induce release of calprotectin (leucocyte L1 protein) from polymorphonuclear cells in vitro.M
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