Seladelpar-sodium-salt-MBX-8025-sodium-salt-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESeladelpar sodium saltCat. No.: HY-19522ASynonyms: MBX-8025 sodium salt; RWJ-800025 sodium salt分式: CHFNaOS分量: 466.45作靶點(diǎn): PPAR作通路: Cell Cycle/DNA Damage儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外

2、實(shí)驗(yàn) DMSO : 50 mg/mL (107.19 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.1439 mL 10.7193 mL 21.4385 mL5 mM 0.4288 mL 2.1439 mL 4.2877 mL10 mM 0.2144 mL 1.0719 mL 2.1439 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可

3、靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.36 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.36 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn o

4、ilSolubility: 2.5 mg/mL (5.36 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Seladelpar sodium salt (MBX-8025)種具有服活性的、選擇性的 PPAR 激動(dòng)劑，EC50 值為 2 nM。它對(duì) PPAR 的選擇性分別對(duì) PPAR 和 PPAR 的 750 和 2500 多倍。IC50 & Target PPAR-2 nM (EC50)體外研究 MBX-8025 is an orally active, po

5、tent (EC50=2 nM), and specific (750-fold and 2500-fold compared withPPAR or PPAR receptors, respectively) PPAR agonist being developed as a lipid-altering agent 2 3.體內(nèi)研究 In atherogenic diet-fed Wt mice, administration of Seladelpar sodium salt reduces body weight by 18%(Pfoz/foz mice. Seladelpar sod

6、ium salt lowers serum alanine aminotransferase (ALT) levels in foz/foz mice(PWt mice. Seladelpar sodium salt normalizes serum cholesterol and decreases triglycerides in bothgenotypes (Pfoz/foz mice (P 4.PROTOCOLCell Assay 3 Human PPAR, PPAR and PPAR activity is monitored in transiently transfected c

7、ells treated withincreasing concentrations of MBX-8025 (0.1 nM, 1 nM, 10 nM, 100, nM, 1000 nM) in comparison withreference compounds (0.1 nM-1 M) for individual subtypes. The PPAR subtype selectivity of MBX-8025 isevaluated in a cell-based GAL4 reporter assay system 3.MCE has not independently confi

8、rmed the accuracy of these methods. They are for reference only.Animal Mouse: From weaning (week 4), Alms1 mutant (foz/foz) NOD.B10 mice or Wt littermates (female mice in bothAdministration 4 groups) are fed an atherogenic diet (23% fat, 0.2% cholesterol and 45% simple carbohydrate; 4.78 kcal/gdiges

9、tible energy) ad libitum for 16 weeks, after which groups are randomized (n=8 to 12 mice/group) toonce-a-day oral administration (by gavage) for 8 weeks of Seladelpar sodium salt (10 mg/kg in 1%methylcellulose) or vehicle (controls). Animals are housed under 12-hour light/dark cycle and constanttemp

10、erature of 22C and receive maximal humane care 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Sahebkar A, et al. New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic

11、 fatty liver disease. Expert Opin Pharmacother. 2014 Mar;15(4):493-503.2. Bays HE, et al. MBX-8025, a novel peroxisome proliferator receptor-delta agonist: lipid and other metabolic effects in dyslipidemicoverweight patients treated with and without atorvastatin. J Clin Endocrinol Metab. 2011 Sep;96

12、(9):2889-97.3. Choi YJ, et al. Effects of the PPAR- agonist MBX-8025 on atherogenic dyslipidemia. Atherosclerosis. 2012 Feb;220(2):470-6.4. Haczeyni F, et al. The selective peroxisome proliferator-activated receptor-delta agonist seladelpar reverses nonalcoholic steatohepatitispathology by abrogating lipotoxicity in diabetic obese mice. Hepatol Commun. 2017 Jul 31;1(7):663-674.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECau