SMILES string
OC(COC1=C(C=C(C=C1)SC[C@H](OCC)COC2=CC=C(C=C2)C(F)(F)F)C)=O
assay
≥98% (HPLC)
form
(liquid, semi-solid, solid or powder)
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Application
Seladelpar has been used as a PPARδ agonist to study its role in reducing bile acid synthesis in hepatocytes.
Biochem/physiol Actions
Seladelpar (MBX-8025) is an orally active, potent and selective Peroxisome proliferator–activated receptor delta (PPAR-δ) agonist (EC50 = 2 nM post 24h treatment using HEK293 PPARβ/δ reporter cells) with >750- and >2500-fold higher potency over that of PPAR-α and PPAR-γ, respectively. Seladelpar reduces ethanol-induced liver disease by restoring gut barrier function and bile acid homeostasis in mice in vivo (10 mg/kg/d via liquid diet). Seladelpar plays a significant role in regulating bile acid metabolism and inflammation. By activating PPARδ, seladelpar promotes fatty acid oxidation and reduces lipid accumulation in the liver, which is predominantly observed in primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH). PPARδ activation also results in the downregulation of bile acid synthesis by reducing the expression of cholesterol 7 alpha-hydroxylase (CYP7A1), a key enzyme in bile acid synthesis. Seladelpar also enhances the signaling of fibroblast growth factor 21 (FGF21), contributing to its anti-inflammatory effects.
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Tetsuya Kouno et al.
The Journal of biological chemistry, 298(7), 102056-102056 (2022-05-24)
Peroxisome proliferator-activated receptor delta (PPARδ) agonists have been shown to exert beneficial effects in liver disease and reduce total bile acid levels. The mechanism(s) whereby PPARδ agonism reduces bile acid levels are, however, unknown, and therefore the aim of the
Huikuan Chu et al.
Translational research : the journal of laboratory and clinical medicine, 227, 1-14 (2020-06-20)
Alcohol-associated liver disease is accompanied by dysregulation of bile acid metabolism and gut barrier dysfunction. Peroxisome proliferator-activated receptor-delta (PPARδ) agonists are key metabolic regulators and have anti-inflammatory properties. Here, we evaluated the effect of the selective PPAR-delta agonist seladelpar (MBX-8025)
Fahrettin Haczeyni et al.
Hepatology communications, 1(7), 663-674 (2018-02-07)
Lipotoxicity associated with insulin resistance is central to nonalcoholic steatohepatitis (NASH) pathogenesis. To date, only weight loss fully reverses NASH pathology, but mixed peroxisome proliferator-activated receptor-alpha/delta (PPAR-α/δ) agonists show some efficacy. Seladelpar (MBX-8025), a selective PPAR-δ agonist, improves atherogenic dyslipidemia.
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