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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Seladelpar (lysine dihydrate)
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Biological Activity
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PPARδ 2 nM (EC50) |
IL-31 |
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
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)
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.
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.
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 |
|---|---|---|---|---|---|
| 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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- 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