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Seladelpar

Catalog No. T4628   CAS 851528-79-5
Synonyms: MBX 8025

Seladelpar (MBX 8025) has been used in trials studying the treatment of Hyperlipidemia.

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Seladelpar Chemical Structure
Seladelpar, CAS 851528-79-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
2 mg In stock $ 44.00
5 mg In stock $ 72.00
10 mg In stock $ 122.00
25 mg In stock $ 228.00
50 mg In stock $ 396.00
100 mg In stock $ 593.00
500 mg In stock $ 1,250.00
1 mL * 10 mM (in DMSO) In stock $ 90.00
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Purity: 99.18%
Purity: 99.07%
Purity: 98.39%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Seladelpar (MBX 8025) has been used in trials studying the treatment of Hyperlipidemia.
Targets&IC50 PPARδ:2 nM (EC50), PPARα:1600 nM (EC50)
In vitro Seladelpar (MBX-8025) is an orally administered, highly potent (2 nM), and selective PPAR-δ agonist, exhibiting more than 750-fold and 2500-fold specificity over PPAR-α and PPAR-γ receptors, respectively. Developed as a lipid-modifying agent, it demonstrates significant efficacy in improving insulin resistance, diabetes, and atherogenic dyslipidemia by targeting human PPAR-δ with a 50% effective concentration of 2 nM, compared to 1,600 nM for PPAR-α.
In vivo Female Alms1 mutant (foz/foz) mice and their wild-type siblings were subjected to an atherogenic diet for 16 weeks post-weaning. Subsequently, groups (n=8-12) were randomized to receive either 10 mg/kg Seladelpar or a vehicle (1% methylcellulose) via gavage for 8 weeks. Seladelpar efficiently normalized hyperglycemia, hyperinsulinemia, and glucose disposal in foz/foz mice without significantly affecting body weight. It halved serum alanine aminotransferase levels, which ranged from 300-600 U/L in vehicle-treated foz/foz mice, and corrected serum lipid profiles as well as hepatic concentrations of free cholesterol and other lipotoxic lipids elevated in these mice compared to wild-type. These corrections led to the abolition of hepatocyte ballooning and apoptosis, marked reductions in steatosis and liver inflammation, and improved liver fibrosis. Vehicle-treated foz/foz mice had an average nonalcoholic fatty liver disease (NAFLD) activity score of 6.9, indicative of nonalcoholic steatohepatitis (NASH), which Seladelpar entirely reversed (NAFLD activity score reduced to 3.13). In wild-type mice fed an atherogenic diet, Seladelpar administration resulted in an approximate 18% reduction in body weight (P<0.05). However, it had a minimal impact on the body weight of atherogenic diet-fed foz/foz mice. These mice developed severe metabolic disruptions after 16 weeks, which Seladelpar significantly ameliorated (P<0.05). Following an intraperitoneal glucose challenge, blood glucose levels were significantly lower in Seladelpar-treated foz/foz mice compared to vehicle-treated ones (P<0.05), demonstrating Seladelpar's substantial improvement on glucose handling, an effect similarly observed in wild-type mice on an atherogenic diet (P<0.05).
Animal Research From weaning (week 4), Alms1 mutant (foz/foz) NOD.B10 mice or Wt littermates (female mice in both groups) are fed an atherogenic diet (23% fat, 0.2% cholesterol and 45% simple carbohydrate; 4.78 kcal/g digestible energy) ad libitum for 16 weeks, after which groups are randomized (n=8-12 mice/group) to once-a-day oral administration (by gavage) for 8 weeks of Seladelpar (10 mg/kg in 1% methylcellulose) or vehicle (controls). Animals are housed under 12-hour light/dark cycle and constant temperature of 22°C and receive maximal humane care[2].
Synonyms MBX 8025
Molecular Weight 444.46
Formula C21H23F3O5S
CAS No. 851528-79-5

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (22.5 mM)

TargetMolReferences and Literature

1. 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. 2. 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.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Transcription Factor-Targeted Compound Library NO PAINS Compound Library Anti-Cancer Compound Library Anti-Diabetic Compound Library Anti-Obesity Compound Library Bioactive Compounds Library Max Human Metabolite Library

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Keywords

Seladelpar 851528-79-5 DNA Damage/DNA Repair Metabolism PPAR MBX-8025 Peroxisome proliferator-activated receptors active atherogenic diabetes orally MBX8025 inhibit dyslipidemia resistance MBX 8025 insulin Inhibitor inhibitor

 

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