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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(2681)

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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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