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GW-0742 Specifications
Other name: GW610742, Fitorine
CAS No.: 317318-84-6
MF: C21H17F4N03S2
Appearance: White powder
Purity: 99%
Dosage: 20-30mg per day
GW-0742 Description
GW 0742 activates AMP-activated protein kinase and simulates glucose uptake in skeletal muscle tissue,and GW501516 has been demonstrated to reverse metabolic abnormalities in obese men with pre-diabetic metabolic syndrome , most likely by stimulating fatty acid oxidation
GW0742 has been proposed as a potential treatment for obesity and related conditions, especially when used in conjunction with a synergistic compound AlCAR, as the combination has been shown to significantly increase exercise endurance in human.
How GW0742 Works
The highest antagonist activity for Gw0742 was found for VDR and the androgen receptor (AR). surprisingly,GW0742 behaved as PPAR antagonist activating transcription at lower concentration and inhibiting this effect at higher concentrations. A unique spectroscopic property of GW0742 was identified as well. in the presence of Dramamine-derived molecules,GW0742+ increased fluorescence intensity and fluorescence polarization at an excitation wavelength of 595 nm and emission wavelength of 615 nm in a dose dependent manner.
The GW0742 inhibited NR-co activator binding resulted in a reduced expression of five different NR target genes in LNCaP cells in the presence of agonist. Especially VDR target genes CYP24A1, lGFBp-3 and TRPV6 were negatively regulated by GW0742. GW-0742 is the first VDR ligand inhibitor lacking the secosteroid structure of VDR and antagonists. Nevertheless, the VDR-meditated downstream process of cell differentiation was antagonized by Gw0742 in H-60 cells that were pretreated with the endogenous VDR agonist 1,25-dihydroxyvitamin D3.
