|Place of Origin:||CHINA|
|Certification:||GMP , ISO 9001:2008|
|Minimum Order Quantity:||10g|
|Packaging Details:||Disguised Package|
|Delivery Time:||2 Working Days|
|Payment Terms:||Bank Transfer - Bitcoin - Western Union - MoneyGram|
|Supply Ability:||100 KG/Month|
|Appearance:||Yellow Powder||Usage:||Muscle Gaining|
|Shipping Method:||EMS, HKEMS, FEDEX, DHL, UPS, Aramex, ETC||Color:||Yellow|
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|Synonyms||GW0742;[4-[[[2-[3-FLUORO-4-(TRIFLUOROMETHYL)PHENYL]-4-METHYL-5-THIAZOLYL]METHYL]THIO]-2-METHYLPHENOXY]ACETIC ACID;4-[2-(3-FLUORO-4-TRIFLUOROMETHYL-PHENYL)-4-METHYL-THIAZOL-5-YLMETHYLSULFANYL]-2-METHYL-PHENOXY-ACETIC ACID;4-[[[2-[3-Fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl]methyl]thio]-2-methylphenoxy]AceticAcid;4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl-thiazol-5-ylmethylsulfanyl]- 2-methyl-phenoxy}-acetic acid;Acetic acid, 2-[4-[[[2-[3-fluoro-4-(trifluoroMethyl)phenyl]-4-Methyl-5-thiazolyl]Methyl]thio]-2-Methylphenoxy]-;2-(4-(((2-(3-Fluoro-4-(trifluoromethyl)phenyl)-4-methylthiazol-5-yl)methyl)thio)-2-methylphenoxy);GW 0742X|
|Appearance||Light Yellow Solid|
|Shipment||EMS, FedEx, TNT, DHL, UPS|
|Delivery||within 1 day after we get the payment|
|Product Categories||AllInhibitors;Inhibitors;Intermediates&FineChemicals;Pharmaceuticals;Intracellular receptor;Inhibitor|
|Usage||A small molecule agonist of the human Peroxisome Proliferator-Activated Recept d (PPAR d). It shows an EC50 of 1.1 nM against PPAR d with 100-fold selectivity over the other human subtypes|
GW 0742 is a selective PPARδ agonist (EC50 = 1.1 nM) that exhibits 1,000-fold selectivity over the other human PPAR subtypes. GW 0742 exhibits time-dependent neuroprotection in low KCl-induced apoptosis in cerebellar granule neuronal cultures. Despite the neuroprotective properties observed, prolonged (48h) incubation with GW 0742 produced significant inherent toxicity. This cell death was determined to be apoptotic as identified with the TUNEL assay.
GW-0742 shows activity against hPPARα, hPPARγ and hPPARδ with EC50 of 1.1 μM, 2 μM and 1 nM, respectively, in cell based transactivation assay. GW-0742 (0.2 μM and 1 μM) significant increases in reporter activity of PPARβ/δ in N/TERT-1 keratinocytes. GW0742 (1 μM) results in significant inhibition in the average number of N/TERT-1 keratinocytes.
GW-0742 at 100 μM produces a pronounced increase in c-Jun expression at 6 hours in cerebellar granule neuron cultures. GW0742 at 100 μM increases PPARα-mediated transactivation dependent on the presence of 1.5% BSA in MCF-7 cells.
GW0742 is a synthetic high affinity PPAR β/δ agonist, and its possible role in preventing the advance of inflammatory and apoptotic processes induced by bleomycin, that long-term leads to the appearance of pulmonary fibrosis. Our data showed that GW0742-treatment (0.3 mg/Kg, 10 percent DMSO, i.p.) has therapeutic effects on pulmonary damage, decreasing many inflammatory and apoptotic parameters detected by measurement of: 1) cytokine production; 2) leukocyte accumulation, indirectly measured as decrease of myeloperoxidase (MPO) activity; 3) IkBα degradation and NF-kB nuclear translocation; 4) ERK phosphorylation; 5) stress oxidative by NO formation due to iNOS expression; 6) nitrotyrosine and PAR localization; 7) the degree of apoptosis, evaluated by Bax and Bcl-2 balance, FAS ligand expression and TUNEL staining. Taken together, our results clearly show that GW0742 reduces the lung injury and inflammation due to the intratracheal BLEO--instillation in mice.
GW0742 is a synthetic, potent and selective PPAR-β/δ agonist. PPARs are ligand-dependent transcription factors which are involved in many physiological processes, such as inflammation and energy homeostasis. PPAR-β/δ is one of three PPARs in the nuclear hormone receptor superfamily that are collectively involved in the control of lipid homoeostasis among other functions. GW0742 can attenuate the increase of PARP activity that caused by SAO shock. GW0742 is also able to prevent radiation-induced brain injury in C57Bl/6 wild-type (WT) and PPARδ knockout (KO) mice. Dietary GW0742 can prevent the acute increase in IL-1β mRNA and ERK phosphorylation measured at 3 h after a single 10-Gy dose of WBI as well as the increase in the number of activated hippocampal microglia 1 week after WBI.
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