Highly Selective GW0742 99% Natural Nutrition Supplements CAS 317318-84-6

Highly Selective GW0742 99% Natural Nutrition Supplements CAS 317318-84-6

 

Quick Details for GW0742

Product Name: GW0742
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
CAS: 317318-84-6
MF: C21H17F4NO3S2
MW: 471.49
Product Categories: All Inhibitors;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Intracellular receptor;Inhibitor
Melting point : 134.5-135.5 °C
Storage temp. : 2-8°C
Chemical Properties : White Solid
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
Usage : A small molecule agonist of the human Peroxisome Proliferator-Activated Recept δ (PPAR δ). It shows an EC50 of 1.1 nM against PPAR δ with 100-fold selectivity over the other human subtypes.

 

GW0742 Description

GW0742 shows activity aganist hPPARα, hPPARγ and hPPARδ with EC50 of 1.1 μM, 2 μM and 1 nM, respectively, in cell based transactivation assay. GW0742 (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. GW0742 (1 μM) results in an increase in the number of cells in the G1 phase and a decrease in the number of cells in the S phase. GW0742 (1 μM) causes a significant increase in the mRNA encoding ADRP, a known PPARβ/δ target gene, in N/TERT-1 keratinocytes as well as mouse primary keratinocytes. GW0742 (1 μM) results in significantly reduced phosphorylation of retinoblastoma (Rb) and a significantly lower level of p42/44 ERK in N/TERT-1 cells. GW0742 (1 μM) leads to an increase in the mRNA encoding a number of known markers of terminal differentiation including TG-I, SPR1A, K10 and involucrin. GW0742 at 100 μM produces a significant reduction in low-KCl-induced neuronal cell death in cerebellar granule neurons. GW0742 at 100 μM induces a pronounced increase in cell death as measured by LDH release after 48 hr of incubation. GW0742 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.

 

How it works ?

ENDUROBOL is a selective agonist ( activator ) of the PPARδ receptor . It displays high affinity ( Ki = 1 nM ) and potency ( EC50 = 1 nM ) for PPARδ with > 1000 fold selectivity over PPARα and PPARγ .

It activates AMP-activated protein kinase and stimulates glucose uptake in skeletal muscle tissue , and GW 501516 has been demonstrated to reverse metabolic abnormalities in obese men with pre-diabetic metabolic syndrome , most likely by stimulating fatty acid oxidation . It has been proposed as a potential treatment for obesity and related conditions , especially when used in conjunction with a synergistic compound AICAR , as the combination has been shown to significantly increase exercise endurance in human .

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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