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Seladelpar sodium salt

    
10mM in DMSO

源叶(MedMol)
V58381 一键复制产品信息
3026272-26-1
C21H22F3NaO5S
466.45
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
V58381-1ml
10mM in DMSO

¥470.00

货期:3-5天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: Seladelpar (MBX-8025) sodium salt is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM. Seladelpar sodium salt shows more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively. Seladelpar sodium salt hydrochloride can be used for the study of primary biliary cholangitis.
靶点: PPAR-δ:2 nM (EC50)
体外研究: In atherogenic diet-fed Wt mice, administration of Seladelpar sodium salt reduces body weight by ~18% (P<0.05). In contrast, Seladelpar sodium salt produces minimal effect on body weight in atherogenic diet-fed foz/foz mice. Seladelpar sodium salt lowers serum alanine aminotransferase (ALT) levels in foz/foz mice (P<0.05) and similarly (but not significantly) in Wt mice. Seladelpar sodium salt normalizes serum cholesterol and decreases triglycerides in both genotypes (P<0.05). Seladelpar sodium salt abolishes hepatocyte ballooning (P<0.05) and decreases the nonalcoholic fatty liver disease (NAFLD) activity score by ~50%. Seladelpar sodium salt also significantly reduces sirius red-positive areas in foz/foz mice (P<0.05).
体内研究: Seladelpar (MBX-8025) sodium salt is an orally active, potent (EC50=2 nM), and specific (750-fold and 2500-fold compared with PPARα or PPARγ receptors, respectively) PPARδ agonist being developed as a lipid-altering agent[2][3].
参考文献: 1. Sahebkar A, et al. New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic 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 dyslipidemic overweight patients treated with and without atorvastatin. J Clin Endocrinol Metab. 2011 Sep;96(9):2889-97.
3. Choi YJ, et al. Effects of the PPAR-δ 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 steatohepatitis pathology by abrogating lipotoxicity in diabetic obese mice. Hepatol Commun. 2017 Jul 31;1(7):663-674.
 
保存条件: -80°C 12个月; -20°C 6个月, 干燥
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.144 ml 10.719 ml 21.439 ml
5 mM 0.429 ml 2.144 ml 4.288 ml
10 mM 0.214 ml 1.072 ml 2.144 ml
50 mM 0.043 ml 0.214 ml 0.429 ml
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参考文献

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