Seladelpar sodium salt (MBX-8025) is an orally bioactive, selective PPARδ agonist/activator with EC50 of 2 nM. Its selectivity for PPARδ is over 750 and 2500 times that for PPARα and PPARγ, respectively.

Physicochemical Properties

Molecular Formula	C21H22F3NAO5S
Molecular Weight	466.45
CAS #	3026272-26-1
Related CAS #	Seladelpar;851528-79-5
Appearance	White to off-white solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	PPAR-δ 2 nM (EC50)
ln Vitro	MBX-8025 is a PPARδ agonist that is being developed as a lipid-altering therapy. It is orally active, powerful (EC50=2 nM), and selective (750-fold and 2500-fold compared with PPARα or PPARγ receptors, respectively).
ln Vivo	Seladelpar sodium salt injection results in a ~18% (P<0.05) reduction in body weight in Wt mice fed an atherogenic diet. On the other hand, Seladelpar sodium salt had very little influence on body weight in mice fed an atherogenic diet (foz/foz). Serum alanine aminotransferase (ALT) levels are lowered in foz/foz mice (P<0.05) and Wt mice in a comparable (though not statistically significant) manner by seladelpar sodium salt. In both genotypes, seladelpar sodium salt lowers triglycerides and normalizes blood cholesterol (P<0.05). Hepatocyte ballooning is eliminated by salt (P<0.05), and the nonalcoholic fatty liver disease (NAFLD) activity score is reduced by approximately 50%. Additionally, in foz/foz mice, seleadelpar sodium salt dramatically lowers sirius red-positive regions (P<0.05)[4].
References	[1]. New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease. Expert Opin Pharmacother. 2014 Mar;15(4):493-503. [2]. MBX-8025, a novel peroxisome proliferator receptor-delta agonist: lipid and other metabolic effects in dyslipidemic overweight patients treated with and without atorvastatin. J Clin Endocrinol Metab. 2011 Sep;96(9):2889-97. [3]. Effects of the PPAR-δ agonist MBX-8025 on atherogenic dyslipidemia. Atherosclerosis. 2012 Feb;220(2):470-6. [4]. The selective peroxisome proliferator-activated receptor-delta agonist seladelpar reverses nonalcoholic steatohepatitis pathology by abrogating lipotoxicity in diabetic obese mice. Hepatol Commun. 2017 Jul 31;1(7):663-674.

Solubility Data

Solubility (In Vitro)

DMSO :~50 mg/mL (~107.19 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.36 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 (5.36 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (5.36 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	2.1439 mL	10.7193 mL	21.4385 mL
	5 mM	0.4288 mL	2.1439 mL	4.2877 mL
	10 mM	0.2144 mL	1.0719 mL	2.1439 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.