| Field | Specification |
|---|---|
| Target | |
| Alternative names | MBX-8025 (lysine dihydrate); RWJ-800025 (lysine dihydrate) |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C27H41F3N2O9S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Seladelpar (lysine dihydrate), also known as MBX-8025 (lysine dihydrate) and RWJ-800025 (lysine dihydrate), is an orally active, selective PPAR-δ agonist with an EC50 of 2 nM against hPPAR-δ. It reduces serum IL-31 and bile acid levels and alleviates pruritus symptoms, and it enhances insulin sensitivity, normalizing hyperglycemia, hyperinsulinemia, glucose disposal capacity, serum lipids, and hepatic free cholesterol levels. It also reduces steatosis and hepatic inflammation, improves liver fibrosis, and reverses the pathological changes of non-alcoholic steatohepatitis (NASH), and it is applicable to research related to primary biliary cholangitis and NASH[1][2]. It is supplied as a white to off-white solid (C27H41F3N2O9S, MW 626.68) at 99.51% purity.
Physical & Chemical Properties
| CAS Number | 928821-40-3 |
|---|---|
| Molecular Formula | C27H41F3N2O9S |
| Molecular Weight | 626.68 g/mol |
| Purity | 99.51% |
| Appearance | Solid |
| Color | White to off-white |
| 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 |
| Target | PPARδ, IL-31 |
| Signaling Pathway | Cell Cycle/DNA Damage; Vitamin D Related/Nuclear Receptor; Metabolic Enzyme/Protease; Immunology/Inflammation |
| Solubility | In Vitro: DMSO: 25 mg/mL (39.89 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
[2][1]
|
PPARδ 2 nM (EC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 25 mg/mL (39.89 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (3.99 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (3.99 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (3.99 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vivo
In atherogenic diet-fed obese diabetic foz/foz mice, Seladelpar (10 mg/kg; p.o.; once daily; 8 weeks) lysine dihydrate enhances insulin sensitivity, normalizes dyslipidemia, lowers hepatic lipotoxic lipid levels, and reverses NASH pathology, and also gives beneficial metabolic effects in wild-type littermates[2].
| 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] |
|---|---|
| Dosage | 10 mg/kg |
| Administration | p.o.; once daily; 8 weeks |
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Metabolic flux analysis of bile acid biosynthesis acidic pathway in HepG2 cells reveals CYP8B1 inhibition of azole antifungals. Drug Metab Dispos 2025 Nov;53(11):100168. PMID: 41124962
