Wuhan Zeuschem Ltd.  

Product Name: Sarms Powder Gw0742 / Gw-0742 / Gw610742 for Muscle Building CAS 1196133-39-7 Model NO.: sarms MOQ: 1g Trademark: w/o Transport Package: Safety Package Specification: white powder Origin: China HS Code: 3006601000 Product Description Sarms Powder GW0742 / GW-0742 / GW610742 For Muscle Building CAS 1196133-39-7GW0742 (also known as GW610742) is a PPARδ/β agonist[2][3][4] that is investigated for drug use by GlaxoSmithKline.[5]DEscriptIonSynonymsGW 610742The transcription factor peroxisome proliferator-activated receptor δ (PPARδ) is a member of the superfamily of nuclear hormone receptors and is implicated both in lipid metabolism and in the regulation of genes with potential roles in neurotoxicity. GW 0742 is a selective PPARδ agonist (EC50 = 1.1 nM) that exhibits 1,000-fold selectivity over the other human PPAR subtypes.1 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.2CAS No.:317318-84-6Synonyms:GW 0742;Formula:C21H17F4NO3S2Exact Mass:471.05900Molecular Weight:471.48800PSA:112.96000LogP:6.34050Description:GW0742 is a high affinity PPAR-β/δ agonist reduces lung inflammation induced by bleomycin instillation in mice.A high throughput screening campaign was conducted to identify small molecules with the ability to inhibit the interaction between the vitamin D receptor (VDR) and steroid receptor coactivator 2. These inhibitors represent novel molecular probes to modulate gene regulation mediated by VDR. The peroxisome proliferator-activated receptor δ (PPARδ) agonist GW0742 was among the identified VDR-coactivator inhibitors and has been characterized herein as a pan nuclear receptor antagonist at concentrations higher than 12.1 µM. The highest antagonist activity for GW0742 was found for VDR and the androgen receptor (AR). Surprisingly, GW0742 behaved as PPAR agonist/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 rhodamine-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-coactivator 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, IGFBP-3 and TRPV6 were negatively regulated by GW0742. GW0742 is the first VDR ligand inhibitor lacking the secosteroid structure of VDR ligand antagonists. Nevertheless, the VDR-meditated downstream process of cell differentiation was antagonized by GW0742 in HL-60 cells that were pretreated with the endogenous VDR agonist 1,25-dihydroxyvitamin D3.