Seladelpar (Synonyms: MBX-8025) |
Catalog No.GC19242
One-Click Copy Product Info
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Seladelpar is a potent and selective peroxisome proliferator-activated receptor delta (PPARδ) agonist (EC50=2nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 851528-79-5
Sample solution is provided at 25 µL, 10mM.
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Seladelpar is a potent and selective peroxisome proliferator-activated receptor delta (PPARδ) agonist (EC50=2nM). Seladelpar inhibits bile acid synthesis by activating PPARδ. Seladelpar can be used in research related to primary biliary cholangitis (PBC)[1-4].
In vitro, H69 cholangiocytes were treated with Seladelpar (10nM–10μM) for 22-96 hours. Seladelpar significantly increased the expression of PDK4, ANGPTL4, CPT1A, PLIN2, ACSL1, and ABCA1 in a concentration-dependent manner[5]. Primary mouse hepatocytes and primary human hepatocytes were treated with Seladelpar (0.1–10μM) for 48 hours. Seladelpar significantly reduced the expression of cholesterol 7α-hydroxylase (Cyp7a1/CYP7A1) and induced the expression of fibroblast growth factor 21 (Fgf21/FGF21)[6].
In vivo, Seladelpar (10mg/kg/day) was added to a liquid diet and administered to C57BL/6 mice subjected to ethanol feeding for 4 weeks. Seladelpar significantly reduced ethanol-induced liver injury, lowered plasma ALT and AST levels, alleviated hepatic steatosis and inflammation, and restored bile acid homeostasis and intestinal barrier function[7]. Seladelpar (10mg/kg/day) was orally administered to a non-alcoholic steatohepatitis (NASH) C57BL/6JRj mouse model fed a specific diet for 12 weeks. Seladelpar significantly reduced liver fibrosis[8].
References:
[1] Shukla AK, Misra S. Seladelpar: a comprehensive review of its clinical efficacy and safety in the treatment of primary biliary cholangitis. J Basic Clin Physiol Pharmacol. 2025 Aug 11;36(5):331-337.
[2] Khoury AP, Powell J. Seladelpar for the Treatment of Primary Biliary Cholangitis. Ann Pharmacother. 2025 Oct;59(10):951-958.
[3] Kremer AE, Mayo MJ, Hirschfield GM, et al. Seladelpar treatment reduces IL-31 and pruritus in patients with primary biliary cholangitis. Hepatology. 2024 Jul 1;80(1):27-37.
[4] Hoy SM. Seladelpar: First Approval. Drugs. 2024 Nov;84(11):1487-1495.
[5] Xia Wu, Wen-Yen Chen, Jianguo Song, et al. PPAR-delta activation with seladelpar regulates cholangiocyte inflammation. Journal of Hepatology. 2024 June;6:5-8.
[6] Kouno T, Liu X, Zhao H, et al. Selective PPARδ agonist seladelpar suppresses bile acid synthesis by reducing hepatocyte CYP7A1 via the fibroblast growth factor 21 signaling pathway. J Biol Chem. 2022 Jul;298(7):102056.
[7] Chu H, Jiang L, Gao B, et al. The selective PPAR-delta agonist seladelpar reduces ethanol-induced liver disease by restoring gut barrier function and bile acid homeostasis in mice. Transl Res. 2021 Jan;227:1-14.
[8] Choi YJ, Johnson JD, Lee JJ, et al. Seladelpar combined with complementary therapies improves fibrosis, inflammation, and liver injury in a mouse model of nonalcoholic steatohepatitis. Am J Physiol Gastrointest Liver Physiol. 2024 Feb 1;326(2):G120-G132.
| Cell experiment [1]: | |
Cell lines | H69 cholangiocytes |
Preparation Method | H69 human cholangiocytes were cultured and exposed to varying concentrations and durations of Seladelpar treatment. |
Reaction Conditions | 10nM–10μM; 22-96h |
Applications | Seladelpar significantly increased the expression of PDK4, ANGPTL4, CPT1A, PLIN2, ACSL1, and ABCA1, Seladelpar had a dose-dependent effect. |
| Animal experiment [2]: | |
Animal models | C57BL/6JRj mice |
Preparation Method | Mice were fed an amylin liver diet for 43 weeks to induce on-alcoholic steatohepatitis (NASH) and then treated daily for 12 weeks with Seladelpar. |
Dosage form | 10mg/kg; once a day; orally for 12 weeks |
Applications | Seladelpar resulted in stark reductions in liver fibrosis and improved hepatic steatosis and nonalcoholic fatty liver disease activity score (NAS) compared with vehicle. |
References: | |
| Cas No. | 851528-79-5 | SDF | |
| Synonyms | MBX-8025 | ||
| Canonical SMILES | O=C(O)COC1=CC=C(SC[C@H](OCC)COC2=CC=C(C(F)(F)F)C=C2)C=C1C | ||
| Formula | C21H23F3O5S | M.Wt | 444.46 |
| Solubility | DMSO : 50 mg/mL (107.19 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2499 mL | 11.2496 mL | 22.4992 mL |
| 5 mM | 450 μL | 2.2499 mL | 4.4998 mL |
| 10 mM | 225 μL | 1.125 mL | 2.2499 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)