1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGW0742Cat. No.: HY-13928CAS No.: 317318-84-6Synonyms: GW610742分式: CHFNOS分量: 471.49作靶點: PPAR作通路: Cell Cycle/DNA Damage儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 34 mg/mL (72.11 mM)* mea

2、ns soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.1209 mL 10.6047 mL 21.2094 mL5 mM 0.4242 mL 2.1209 mL 4.2419 mL10 mM 0.2121 mL 1.0605 mL 2.1209 mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內實驗 請根據您的實驗動物和給藥式選擇適當的溶解案，配制前請先配制澄清的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的作液，

3、建議您現現配，當天使；澄清的儲備液可以根據儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.30 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.30 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGIC

4、AL ACTIVITY物活性 GW0742種有效的 PPAR 和 PPAR 激動劑，在蛋質結合實驗中，對 PPAR 的 IC50 值為 1 nM；同時對 PPAR，PPAR 和 PPAR 的 EC50 值分別為 1 nM，1.1 M 和 2 M。IC50 & Target PPAR PPAR PPAR1 nM (EC50) 1.1 M (EC50) 2 M (EC50)體外研究 GW0742 is a potent PPAR and PPAR agonist, with an IC50 of 1 nM for human PPAR, and EC50s of 1nM, 1.1 M and 2

5、M for human PPAR, PPAR, and PPAR respectively 1. GW0742 (100 M) activateshuman PPAR and mouse PPAR in MCF-7 cells. GW0742 (100 M) significantly reduces low-KCl-inducedapoptosis of cerebellar granule neurons. GW0742 shows no obvious inherent toxicity on cerebellar granuleneuronal cells after treatmen

6、t of 3-100 M for 24 h, but induces increased cell death at 100 M after 48 hr oftreatment. Moreover, GW0742 (100 M) increases c-Jun expression in cerebellar granule neuron culturesobserved at 6 hr 2. GW0742 (1 M) induces PPAR protein in neonatal rat cardiomyocytes. GW0742 alsoraises mRNA levels of lo

7、ng-chain acyl-CoA dehydrogenase (LCAD), very long-chain acyl-CoAdehydrogenase (VLCAD), acyl-CoA oxidase 1 (ACOX1), uncoupling protein 3 (UCP3), malonyl-CoAdecarboxylase (MCD), and pyruvate dehydrogenase kinase 4 (PDK4) in neonatal rat cardiomyocytes 4.體內研究 GW0742 (0.3 mg/kg, i.p.) reduces intensity

8、masson-trichrome staining, and attenuates the histological signsin bleomycin instillatio (BLEO)-induced lung injury of mice. GW0742 (0.3 mg/kg, i.p.) also causes a reductionof the BLEO-induced loss body weight, and a decrease of myeloperoxidase (MPO) activity. GW0742 showssignificant inhibition of T

9、NF-a and IL-1 in instilled-mice. GW0742 prevents bleomycin-induced IkB-adegradation, reduces the levels of NF-kB p65 in the lung, and decreases iNOS and p-ERK expression inBLEO-induced mice 3. GW0742 (5 mg/kg/day, i.v.) increases PPAR protein level in the heart of rats.GW0742 also induces the increa

10、se in LCAD, VLCAD, and ACOX1 in the heart of rats 4.PROTOCOLCell Assay 2 The PPAR activator GW0742 and the RXR activator 9-cis-retinoic acid are dissolved in DMSO. The finalDMSO concentration des not exceed 0.5% v/v, and this concentration is used in control wells. For eachculture plate, one row of

11、wells is treated with 500 M glutamate. These wells serve as a positive control andfor normalisation of data. Cell death (toxicity) is assessed by using an assay designed to measure lactatedehydrogenase (LDH) release 2.MCE has not independently confirmed the accuracy of these methods. They are for re

12、ference only.Animal Male CD mice (25-35 g) are housed in a controlled environment and provided with standard rodent chow andAdministration 3 water. Mice are randomized into four experimental groups: bleomycin-treated group: mice are subjected tolung injury induced by intratracheal instillation of bl

13、eomycin and treated daily via intraperitoneal injection withvehicle of GW0742 (10% dimethylsulfoxide (OMSO, 1 mL/kg), 1 h after BLEO instillation (n = 15). GW0742group: identical to bleomycin-treated group but mice are treated daily with GW0742 (0.3 mg/kg, 1h afterBLEO instillation) via intraperiton

14、eal injection (n = 15). Sham-operated mice + vehicle group: animals are2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEsubjected to the identical surgical procedure but receive intratracheal instillation of saline (0.9%) instead ofBLEO and are treated daily with the vehicle of GW0742 (10% dimethyls

15、ulfoxide (DMSO), 1 mL/kg, i.p.), 1 hafter saline instillation (n = 15). Sham-operated mice + GW0742 group: identical to sham + vehicle group butmice are treated daily with GW0742 (0.3 mg/kg, 1 h after saline instillation) via intraperitoneal injection (n =15) 3.MCE has not independently confirmed th

16、e accuracy of these methods. They are for reference only.戶使本產品發表的科研獻 Biochim Biophys Acta Mol Basis Dis. 2018 Oct;1864(10):3322-3338.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Sznaidman ML, et al. Novel selective small molecule agonists for peroxisome proliferator-activate

17、d receptor delta (PPARdelta)-synthesis and biological activity. Bioorg Med Chem Lett. 2003 May 5;13(9):1517-21.2. Smith SA, et al. Effect of the peroxisome proliferator-activated receptor beta activator GW0742 in rat cultured cerebellar granuleneurons. J Neurosci Res. 2004 Jul 15;77(2):240-9.3. Galuppo M, et al. GW0742, a high affinity PPAR-/ agonist reduces lung inflammation induced by bleomycin instillation in mice. Int JImmunopathol Pharmacol. 2010 Oct-Dec;23(4):1033-46.4. Kuo SC, et al. Activation of receptors (PPAR) by agonist (GW0742) may enhance lipid metabolism in