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            PPARα 系列PPARγ 及 PPARδ 系列 抑制劑 /激動(dòng)劑

            2012-11-7  閱讀(2854)

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            Peroxisome proliferator-activated receptor alpha (PPARα) is a member of the nuclear receptor family of ligand-activated transcription factors that heterodimerize with the retinoic X receptor (RXR) to regulate gene expression. PPARα is located primarily in the liver, adipose tissue, kidney, heart, skeletal muscle and large intestine where it is thought to regulate fatty acid synthesis and oxidation, gluconeogenesis, ketogenesis and lipoprotein assembly. The human gene encoding PPARα has been localized to chromosome 22 (22q12-13.1).
             
            Species   Gene Symbol     Gene Accession No.     Protein Accession No.
            Human     PPARA                 NM_001001928          Q07869
            Mouse      Ppara                    NM_011144              P23204
            Rat           Ppara                    NM_013196              P37230
             
            抑制劑
             
             
             
            GW 6471
             
            分子量:635.68     分子式:C35H36F3N3O5
            Solubility:Soluble to 100 mM in DMSO and to 100 mM in ethanol
            Purity:>98 %                10mg ,50mg 規(guī)格
            CAS No:[436159-64-7]         
            Chemical Name:[(2S)-2-[[(1Z)-1-Methyl-3-oxo-3-[4-(trifluoromethyl)phenyl]-1-propenyl]amino]-3-[4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]propyl]-carbamic acid ethyl ester
             
            Sold with the permission of GlaxoSmithKline   過(guò)氧化物酶增殖活化受體α抑制劑 GW6471    PPARα 系列產(chǎn)品
            PPARα抑制劑 that inhibits activation with an IC50 value of 0.24μM.
             
            MK 886
             
            分子量:472.08       分子式:C27H34ClNO2S
            Solubility:Soluble to 5 mM in ethanol and to 100 mM in DMSO
            Purity:>98 %             10mg ,50mg 規(guī)格
            Storage:Store at RT
            CAS No:[118414-82-7]
            Chemical Name: 1-[(4-Chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-α,α-dimethyl-5-(1-methylethyl)-1H-Indole-2-propanoic acid
            別名:L-663,536
            An inhibitor of leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes). Acts by inhibiting 5-lipoxygenase-activating protein (FLAP) (IC50 = 30 nM for inhibition of [125I]-L-691,678 photoaffinity labelling). Also moderay potent PPARα抑制劑 (IC50 = 0.5-1μM). Orally activein vivo.
             
            激動(dòng)劑
             
            GW 7647
            分子量:502.75              分子式:C29H46N2O3S
            Solubility:Soluble to 25 mM in ethanol and to 100 mM in DMSO      
            Purity:>99 %                 10mg ,50mg 規(guī)格
            CAS No:[265129-71-3]
            Chemical Name: 2-[[4-[2-[[(Cyclohexylamino)carbonyl](4-cyclohexylbutyl)amino]ethyl]phenyl]thio]-2-methylpropanoic acid
            Potent and highly selective PPARαagonist (EC50 values are 6, 1100 and 6200 nM for human PPARα, PPARγand PPARδreceptors respectively). Modulates oleate metabolism and mitochondrial enzyme gene expression in mature myotubulesin vitro. Has lipid-lowering effects following oral administrationin vivo. Reduces NO production in macrophages; exhibits anti-inflammatory properties
             
            Fenofibrate
            分子量:360.83         分子式:C20H21ClO4
            Solubility:Soluble to 100 mM in DMSO and to 100 mM in ethanol
            Purity:>99 %              50mg 規(guī)格
            Storage:Store at RT
            CAS No:[49562-28-9]
            Chemical Name: 2-[4-(4-Chlorobenzoyl)phenoxy]-2-methylpropanoic acid isopropyl ester
            PPARα agonist; hypolipidemic. Attenuates insulin resistance and increases high-density lipoprotein-cholesterol in db/db mice.
             
            296638 [49562-28-9] Fenofibrate 
            294030   Fenofibrate Imp. F (EP): (4-Chlorophenyl)[4-(1-methyl-ethoxy 
            294029   Fenofibrate Imp. E (EP): Ethyl 2-[4-(4-Chlorobenzoyl)-phenox 
            294028   Fenofibrate Imp. D (EP): Methyl 2-[4-(4-Chlorobenzoyl)-pheno 
            294027   Fenofibrate Imp. C (EP): (3RS)-3-[4-(4-Chlorobenzoyl)-phenox 
            294026   Fenofibrate Imp. A (EP): (4-Chlorophenyl)(4-hydroxyphenyl)me 
            294025   Fenofibrate 
            290762   Fenofibrate impurity G 
            290761   Fenofibrate impurity B 
            290760   Fenofibrate impurity A 
            290759   Fenofibrate 
            288620 [49562-28-9] Fenofibrate 
            261137   Fenofibrate-d6 
            261136 49562-28-9 Fenofibrate 
            259465   Dihydro Fenofibrate-d6 
            259464 61001-99-8 Dihydro Fenofibrate 
            257408 856676-23-8 Choline Fenofibrate 
             
             
            Oleylethanolamide
            分子量:325.53           分子式:C20H39NO2
            Purity:>99 %              10mg ,50mg 規(guī)格
            Storage:Store at +4°C
            CAS No:[111-58-0]
            Chemical Name: (9Z)-N-(2-Hydroxyethyl)-9-octadecenamide
             
            Palmitoylethanolamide
            分子量:299.5           分子式:C18N37NO2
            Solubility:Soluble to 20 mM in DMSO and to 25 mM in ethanol
            Storage:Store at RT       10mg ,50mg 規(guī)格    
            CAS No:[544-31-0]
            別名: PEA            Chemical Name: N-(2-Hydroxyethyl)hexadecanamid
             
            WY 14643
             
            分子量:323.8           分子式:C14H14ClN3O2S
            Solubility:Soluble to 100 mM in DMSO
            Purity:>98 %             10mg ,50mg 規(guī)格    
            Storage:Store at RT
            CAS No:[50892-23-4]
             
            Chemical Name: [[4-Chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio]acetic acid
             
            其它相關(guān)產(chǎn)品:
             
            PPARγ
            Peroxisome proliferator-activated receptor gamma (PPARγ) is a member of the nuclear receptor family of ligand-activated transcription factors that heterodimerize with the retinoic X receptor (RXR) to regulate gene expression. PPARγ is located primarily in the adipose tissue, lymphoid tissue, colon, liver and heart and is thought to regulate adipocyte differentiation and glucose homeostasis. PPARγ has been implicated in the pathology of numerous diseases including obesity, diabetes, atherosclerosis and cancer. The human gene encoding PPARγ has been localized to chromosome 3 (3p25).
             
            PPARγ Products
            激動(dòng)劑
             
            Ciglitazone
                Selective PPARγ agonist
            GW 1929 hydrochloride
                Selective PPARγ agonist. Orally active
            LG 100754
            M.Wt:396.56       Formula:C26H36O3
            Solubility:Soluble to 100 mM in DMSO and to 50 mM in ethanol
            Purity:>99 %             10mg ,50mg 規(guī)格
            CAS No:[180713-37-5]
            Chemical Name: (2E,4E,6Z)-3-Methyl-7-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-propoxy-3-naphthalenyl)-2,4,6-octatrienoic acid
            Novel RXR:PPARγagonist; sensitizes PPARγby enhancing its ligand binding activity. Also activates RXR:RAR and RXR:PPARαheterodimers in cotransfection assays. Displays selectivity over other permissive heterodimers such as RXR:LXRαand RXR:BAR/FXR. Exhibits antidiabetic propertiesin vivo.
             
            nTZDpa
                Potent, selective PPARγ partial agonist
            Pioglitazone hydrochlorideNew product
                Selective PPARγ agonist; antidiabetic agent
            15-deoxy-Δ-12,14-Prostaglandin J2
                Endogenous PPARγ agonist
            S26948New productPrices displayed reflect a 25% discount off list price
                Selective PPARγ agonist; antidiabetic agent
            Troglitazone
                Selective PPARγ agonist; antidiabetic agent
             
            Ant激動(dòng)劑:
             
            BADGE
                PPARγ 抑制劑
            GW 9662 Selective PPARγ 抑制劑
            分子量:276.68          
            分子式:C13H19N2O3Cl
            Solubility:Soluble to 25 mM in ethanol
            Purity:>98 %              10mg ,50mg 規(guī)格
            Storage:Store at RT
            CAS No:[22978-25-2]
            Chemical Name: 2-Chloro-5-nitro-N-phenylbenzamide
            Selective PPARγ 抑制劑 (IC50 values are 3.3, 32 and 2000 nM for PPARγ, PPARα and PPARδ respectively). Blocks the inhibition of osteoclast formation induced by IL-4 in the low micromolar range (1-2 μM), therefore is more potent than BADGE . Anticancer, inhibits growth of human mammary tumor cell lines.
             
            SR 202
                Selective PPARγ 抑制劑; antidiabetic and antiobesity agent
            T 0070907
                Highly potent and selective PPARγ 抑制劑
            Other
            Genistein
                PPARγ ligand. Also estrogen receptor ligand and EGFR inhibitor
             
             
            Peroxisome proliferator-activated receptor delta (PPARδ), also known as PPARβ, is a member of the nuclear receptor family of ligand-activated transcription factors that heterodimerize with the retinoic X receptor (RXR) to regulate gene expression.
            PPARδ displays a ubiquitous expression pattern and is thought to regulate placental and gut development, fatty acid oxidation, adaptive thermogenesis, control of cell proliferation and differentiation and tissue repair. The human gene encoding PPARδ has been localized to chromosome 6 (6p21.2).
             
            PPARδ Products
            激動(dòng)劑
            GW 0742
                Highly selective, potent PPARδ agonist
            L-165,041
                Potent PPARδ agonist
            Ant激動(dòng)劑
            GSK 0660
                Selective PPARδ 抑制劑
            GSK 3787
                Potent and selective PPARδ 抑制劑
            Modulators
            Retinoic acid
                Positive modulator of PPARδ. Also retinoic acid receptor agonist
             
            Antibodies and Blocking Peptides
            Anti-PPARδ
                Antibody recognizing PPARδ

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