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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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| 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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| Additional Infomation |
Seladelpar (MBX-8025) has been used in trials studying the treatment of Hyperlipidemia.
Drug Indication Treatment of primary biliary cholangitis |
| Molecular Formula |
C21H23F3O5S
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|---|---|
| Molecular Weight |
444.464535951614
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| Exact Mass |
444.121
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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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| PubChem CID |
11236126
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| Appearance |
Colorless to light yellow liquid
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
557.5±50.0 °C at 760 mmHg
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| Flash Point |
291.0±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.554
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| LogP |
6.16
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
30
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| Complexity |
511
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O(C1C=CC(SC[C@H](OCC)COC2C=CC(C(F)(F)F)=CC=2)=CC=1C)CC(=O)O
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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.
A 12-week, double-blind, randomized, placebo-controlled, Phase 2 study to evaluate the effects of two doses of MBX-8025 in subjects with Primary Biliary Cirrhosis (PBC) and an inadequate response to ursodeoxycholic acid (UDCA).
CTID: null
Phase: Phase 2 Status: Prematurely Ended, Completed
Date: 2015-11-11
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