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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Seladelpar (formerly MBX-8025 and RWJ-800025) is a novel, orally bioactive and selective peroxisome proliferator-activated receptor (PPAR)-δ receptor agonist with anti-cholestatic effects. Its EC50 of 2 nM indicates that it inhibits PPAR-δ. Seladelpar acts as an anti-inflammatory and anti-fibrotic agent through PPAR-delta agonism. Additionally, this method raises lipid metabolism and lowers bile acids. Phase 3 clinical trials are currently being conducted on selegelapar. Treatment for dyslipidemia, metabolic syndrome, type 2 diabetes, and non-alcoholic steatohepatitis may involve the use of selazelpar.
Targets |
PPAR-δ (EC50 = 2 μM); PPAR-α (EC50 = 1600 μM)
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ln Vitro |
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ln Vivo |
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Animal Protocol |
Mice: Atherogenic diet (23 percent fat, 0.2 percent cholesterol, and 45 percent simple carbohydrate; 4.78 kcal/g digestible energy) is fed ad libitum to Alms1 mutant (foz/foz) NOD.B10 mice or Wt littermates (female mice in both groups) from the time of weaning (week 4). Following this, groups are randomized (n=8–12 mice/group) to once-daily oral administration (by gavage) of Seladelpar (10 mg/kg in 1% methylcellulose) or vehicle (controls) for 8 weeks. Animals are kept in housing with a 12-hour light/dark cycle, a constant temperature of 22°C, and the highest level of humane treatment[2].
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References |
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Molecular Formula |
C21H23F3O5S
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Molecular Weight |
444.464535951614
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Exact Mass |
444.12
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Elemental Analysis |
C, 56.75; H, 5.22; F, 12.82; O, 18.00; S, 7.21
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CAS # |
851528-79-5
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Related CAS # |
Seladelpar sodium salt
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Appearance |
Solid powder
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SMILES |
CCO[C@H](COC1=CC=C(C=C1)C(F)(F)F)CSC2=CC(=C(C=C2)OCC(=O)O)C
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InChi Key |
JWHYSEDOYMYMNM-QGZVFWFLSA-N
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InChi Code |
InChI=1S/C21H23F3O5S/c1-3-27-17(11-28-16-6-4-15(5-7-16)21(22,23)24)13-30-18-8-9-19(14(2)10-18)29-12-20(25)26/h4-10,17H,3,11-13H2,1-2H3,(H,25,26)/t17-/m1/s1
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Chemical Name |
2-[4-[(2R)-2-ethoxy-3-[4-(trifluoromethyl)phenoxy]propyl]sulfanyl-2-methylphenoxy]acetic acid
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Synonyms |
MBX-8025; RWJ800025; MBX 8025; RWJ 800025; MBX8025; RWJ-800025
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~100 mg/mL (~225 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2499 mL | 11.2496 mL | 22.4992 mL | |
5 mM | 0.4500 mL | 2.2499 mL | 4.4998 mL | |
10 mM | 0.2250 mL | 1.1250 mL | 2.2499 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04950764 | Recruiting | Drug: Seladelpar 10 mg or less Drug: Seladelpar 10 mg |
Compensated Cirrhosis Hepatic Impairment |
CymaBay Therapeutics, Inc. | September 17, 2021 | Phase 1 |
NCT06051617 | Recruiting | Drug: Seladelpar 10 mg Drug: Placebo |
Primary Biliary Cholangitis | CymaBay Therapeutics, Inc. | September 7, 2023 | Phase 3 |
NCT06060665 | Recruiting |
Drug: Seladelpar 10 mg Drug: Placebo |
Primary Biliary Cholangitis | CymaBay Therapeutics, Inc. | September 5, 2023 | Phase 3 |
NCT03301506 | Recruiting | Drug: Seladelpar 5 mg Capsule Drug: Seladelpar 10 mg Capsule |
Primary Biliary Cirrhosis | CymaBay Therapeutics, Inc. | December 12, 2017 | Phase 3 |
NCT03602560 | Completed | Drug: seladelpar 5-10 mg Drug: seladelpar 10 mg |
Primary Biliary Cholangitis | CymaBay Therapeutics, Inc. | October 1, 2018 | Phase 3 |
Effects of MBX-8025 on LDL-C by baseline lipid level (tertile) compared with placebo, with or without ATV 20 mg/d. J Clin Endocrinol Metab . 2011 Sep;96(9):2889-97. td> |
Effects of MBX-8025 on TG levels by baseline TG (tertile) compared with placebo, with or without ATV 20 mg/d. J Clin Endocrinol Metab . 2011 Sep;96(9):2889-97. td> |
Effects of MBX-8025 with or without ATV 20 mg on the percentage of subjects with metabolic syndrome compared with placebo and ATV alone. *, P < 0.05 vs. placebo and vs. ATV; **, P < 0.01 vs. placebo and vs. ATV. P values for pairwise treatment comparisons were estimated from logistic regression. J Clin Endocrinol Metab . 2011 Sep;96(9):2889-97. td> |
Effects of MBX‐8025 on body weight, hyperglycemia, hyperinsulinemia, serum ALT, cholesterol, and triglyceride in atherogenic diet–fed foz/foz and Wt mice. Hepatol Commun . 2017 Jul 31;1(7):663-674. td> |
Effects of MBX‐8025 on hepatocyte apoptosis, proliferation, fibrosis, and liver inflammation in atherogenic diet–fed foz/foz and Wt mice. Hepatol Commun . 2017 Jul 31;1(7):663-674. td> |