Seladelpar (lysine dihydrate)
Based on 1 publication(s) in Google Scholar
Seladelpar Lysine dihydrate (MBX-8025 lysine dihydrate) is an orally active, selective PPAR-δ agonist with an EC50 of 2 nM against hPPAR-δ. Seladelpar Lysine dihydrate reduces serum IL-31 and bile acid levels. It alleviates pruritus symptoms. Seladelpar Lysine dihydrate enhances insulin sensitivity, normalizes levels of hyperglycemia, hyperinsulinemia, glucose disposal capacity, serum lipids and hepatic free cholesterol. It reduces steatosis, hepatic inflammation and improves liver fibrosis. Seladelpar Lysine dihydrate reverses the pathological changes of non-alcoholic steatohepatitis (NASH). It is applicable to research related to primary biliary cholangitis and non-alcoholic steatohepatitis (NASH).
For research use only. We do not sell to patients.
- Purity : 99.51%
- CAS No.: 928821-40-3
- Formula: C27H41F3N2O9S
- Molecular Weight:626.68
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Seladelpar (lysine dihydrate)
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Biological Activity
Description
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PPARδ 2 nM (EC50) |
IL-31 |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Alms1 mutant (foz/foz) NOD.B10 (female, fed atherogenic diet from weaning for 16 weeks to induce obesity, diabetes, dyslipidemia, NASH); wild-type (Wt) littermates (female, fed atherogenic diet from weaning for 16 weeks)[2]
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Dosage:10 mg/kg
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Administration:p.o.; once daily; 8 weeks
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Result:Normalized hyperglycemia, hyperinsulinemia, and whole-body insulin resistance in foz/foz mice.
Reduced peak blood glucose and lowered the area under the blood glucose disappearance curve during glucose tolerance testing in foz/foz mice.
Reduced serum alanine aminotransferase by 50% in foz/foz mice.
Normalized serum cholesterol and reduced serum triglycerides in foz/foz mice.
Profoundly reduced hepatic total neutral lipids, triglycerides, diacylglycerol, total fatty acids, free cholesterol, and cholesteryl esters in foz/foz mice.
Halved the steatosis score (from 3.00 to 1.88) in foz/foz mice.
Decreased the nonalcoholic fatty liver disease (NAFLD) activity score.
Normalized hepatocyte apoptosis to Wt levels in foz/foz mice.
Suppressed hepatocyte proliferation to Wt levels in foz/foz mice.
Significantly reduced liver fibrosis (sirius red-positive collagen area) in foz/foz mice.
Reduced hepatic macrophage crown-like structures in foz/foz mice.
Chemical Information
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CAS No. 928821-40-3
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Appearance Solid
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Molecular Weight 626.68
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Formula C27H41F3N2O9S
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Color White to off-white
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SMILES
N[C@@H](CCCCN)C(O)=O.O=C(O)COC1=CC=C(SC[C@H](OCC)COC2=CC=C(C(F)(F)F)C=C2)C=C1C.O.O
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Synonyms
MBX-8025 (lysine dihydrate); RWJ-800025 (lysine dihydrate)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Drug Metab Dispos
Metabolic flux analysis of bile acid biosynthesis acidic pathway in HepG2 cells reveals CYP8B1 inhibition of azole antifungals. [Abstract]2025 Nov;53(11):100168. PMID: 41124962
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (39.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Liver Histomorphometry
Liver histomorphometry is a quantitative histological approach used to measure structural alterations in hepatic tissue, including parenchymal loss, steatosis, fibrosis, and vascular remodeling, by combining stained tissue section analysis with stereological or computerized image-based measurements. Classical morphometric frameworks quantify volume fractions of liver compartments and fibrotic regions using systematic sampling and image analysis, enabling objective comparison of pathological changes across experimental groups. These approaches are widely applied in liver cirrhosis and fibrosis studies to reduce subjectivity in histological scoring and improve reproducibility of tissue evaluation. Recent methodological advances integrate automated image analysis and radiomics-based extraction of histological features from standard liver stains (e. g. , H&E and fibrotic stains), enabling quantitative correlation between morphometric features and fibrosis stages in non-alcoholic fatty live
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Kremer AE, et al. Seladelpar treatment reduces IL-31 and pruritus in patients with primary biliary cholangitis. Hepatology. 2024;80(1):27-37. [Content Brief]
[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;1(7):663-674. Published 2017 Jul 31. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.5957 mL | 7.9786 mL | 15.9571 mL | 39.8928 mL |
| 5 mM | 0.3191 mL | 1.5957 mL | 3.1914 mL | 7.9786 mL | |
| 10 mM | 0.1596 mL | 0.7979 mL | 1.5957 mL | 3.9893 mL | |
| 15 mM | 0.1064 mL | 0.5319 mL | 1.0638 mL | 2.6595 mL | |
| 20 mM | 0.0798 mL | 0.3989 mL | 0.7979 mL | 1.9946 mL | |
| 25 mM | 0.0638 mL | 0.3191 mL | 0.6383 mL | 1.5957 mL | |
| 30 mM | 0.0532 mL | 0.2660 mL | 0.5319 mL | 1.3298 mL |
Seladelpar (lysine dihydrate) Related Classifications
HY-19522C Related Classifications
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Keywords
- Seladelpar (lysine dihydrate)
- 928821-40-3
- MBX-8025 lysine dihydrate
- RWJ-800025 lysine dihydrate
- PPAR
- Interleukin Related
- bile acid
- PPAR-a
- peroxisome proliferator-activated receptor-delta
- interleukin-31
- PPAR-delta
- hepatocyte
- foz/foz mice
- primary biliary cholangitis
- wild-type littermates
- nonalcoholic steatohepatitis
- Inhibitor
- inhibitor
- inhibit