1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGW 501516Cat. No.: HY-10838CAS No.: 317318-70-0Synonyms: GW 1516; GSK-516分式: CHFNOS分量: 453.5作靶點: PPAR; Autophagy作通路: Cell Cycle/DNA Damage; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗

2、 DMSO : 100 mg/mL (220.51 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.51 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (5.51 mM); Suspended solution; Need ultrasonic3. 請依序添加每種溶劑： 10% D

3、MSO 90% corn oilSolubility: 2.5 mg/mL (5.51 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 GW 501516是PPAR 的激動劑，EC50 值為 1.1 nM。IC50 & Target PPAR1.1 nM (EC50)體外研究 GW 501516 is shown to be the most potent and selective PPAR agonists known with an EC50 of 1.1 nMagainst PPAR and 1000-fold selectivity over th

4、e other human subtypes, PPAR and- 1. GW 501516exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibitspalmitate- and TNF-induced increases in MCP-1 mRNA expression in a dose-dependent manner 3.體內(nèi)研究 GW 501516 causes impaired bone formation, leading to decr

5、eased BMD and deterioration of bone propertiesin OVX rats 2. GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in aprotein-overload mouse nephropathy model 3. GW 501516 treatment enhances running endurance and theproportion of succinate dehydrogenase (SDH)-positive musc

6、le fibres in both trained and untrained mice 4.PROTOCOLCell Assay 3 GW 501516 is dissolved in DMSO. Cells are starved by incubation in 0.2% FCS DMEM for 9 h, then pre-incubated with GW 501516, at a final concentration of 2.5 and 5 M, or 0.05% DMSO as control for 3 hours,followed by stimulation with

7、150 M palmitate bound to 8.0% BSA for 12 h 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats: Female Sprague Dawley rats, 12 weeks of age, are allocated to a sham-operated group and 3 OVXAdministration 23 groups; high-dose GW 501516 (OVX-GW5

8、), low-dose GW 501516 (OVX-GW1), and a control group (OVX-CTR), respectively. Animals receive GW 501516 or vehicle (methylcellulose) daily for 4 months by gavage.Bone mineral density (BMD) is assessed by dual x-ray absorptiometry at the femur, spine, and whole body2.Mice: Mice are randomly allocated

9、 to different groups and receive therapeutic diet and treatment. The GW501516-containing rodent diet is made by evenly adding GW 501516 to the control diet to a finalconcentration of 0.04% w/w. In the control diet, 10% of the total calories are from fat (5.5% from soybean oiland 4.5% from lard) 3.MC

10、E has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Oncol Res. 2019 Apr 8.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Front Pharmacol. 2018 Jun 28;9:648. Harvard Medical School LINCS LIBRARYSee more customer validations on HYPERLINK / www.Me

11、dChemEREFERENCES1. Wei ZL, et al. A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activatedreceptor delta. J Org Chem. 2003 Nov 14;68(23):9116-8.2. Mosti MP, et al. Effects of the peroxisome proliferator-activated receptor (PPAR)- agonist

12、 GW 501516 on bone and muscle inovariectomized rats. Endocrinology. 2014 Jun;155(6):2178-89.3. Yang X, et al. GW 501516, a PPAR agonist, ameliorates tubulointerstitial inflammation in proteinuric kidney disease via inhibition ofTAK1-NFB pathway in mice. PLoS One. 2011;6(9):e25271.4. Chen W, et al. A

13、 metabolomic study of the PPAR agonist GW 501516 for enhancing running endurance in Kunming mice. Sci Rep.2015 May 6;5:9884.5. Ji Y, et al. PPAR/ Agonist GW501516 Inhibits Tumorigenicity of Undifferentiated Nasopharyngeal Carcinoma in C666-1 Cells byPromoting Apoptosis. Front Pharmacol. 2018 Jun 28;9:648.McePdfH