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        1. 上海北諾生物科技有限公司

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          中級(jí)會(huì)員·13年
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          PPARα 系列PPARγ 及 PPARδ 系列 抑制劑 /激動(dòng)劑

          2012-11-7  閱讀(2680)

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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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