Seladelpar-sodium-salt-MBX-8025-sodium-salt-DataSheet-生命科学试剂-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作靶点: PPAR作通路: Cell Cycle/DNA Damage储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外

2、实验 DMSO : 50 mg/mL (107.19 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可

3、靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.36 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.36 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn o

4、ilSolubility: 2.5 mg/mL (5.36 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Seladelpar sodium salt (MBX-8025)种具有服活性的、选择性的 PPAR 激动剂，EC50 值为 2 nM。它对 PPAR 的选择性分别对 PPAR 和 PPAR 的 750 和 2500 多倍。IC50 & Target PPAR-2 nM (EC50)体外研究 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.体内研究 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 您边的抑制剂师www.MedChemECau