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  3. Seladelpar sodium salt

Seladelpar sodium salt (Synonyms: MBX-8025 sodium salt; RWJ-800025 sodium salt)

Cat. No.: HY-19522A Purity: 98.52%
Handling Instructions

Seladelpar sodium salt (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM, showing more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.

For research use only. We do not sell to patients.

Seladelpar sodium salt Chemical Structure

Seladelpar sodium salt Chemical Structure

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10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 490 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Seladelpar sodium salt (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM, showing more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.

IC50 & Target[1]

PPAR-δ

2 nM (EC50)

In Vitro

MBX-8025 is an orally active, potent (EC50=2 nM), and specific (750-fold and 2500-fold compared with PPARα or PPARγ receptors, respectively) PPARδ agonist being developed as a lipid-altering agent[2][3].

In Vivo

In atherogenic diet-fed Wt mice, administration of Seladelpar sodium salt reduces body weight by ~18% (P<0.05). In contrast, Seladelpar sodium salt produces minimal effect on body weight in atherogenic diet-fed foz/foz mice. Seladelpar sodium salt lowers serum alanine aminotransferase (ALT) levels in foz/foz mice (P<0.05) and similarly (but not significantly) in Wt mice. Seladelpar sodium salt normalizes serum cholesterol and decreases triglycerides in both genotypes (P<0.05). Seladelpar sodium salt abolishes hepatocyte ballooning (P<0.05) and decreases the nonalcoholic fatty liver disease (NAFLD) activity score by ~50%. Seladelpar sodium salt also significantly reduces sirius red-positive areas in foz/foz mice (P<0.05)[4].

Clinical Trial
Molecular Weight

466.45

Formula

C₂₁H₂₂F₃NaO₅S

SMILES

O=C([O-])COC1=CC=C(SC[[email protected]](OCC)COC2=CC=C(C(F)(F)F)C=C2)C=C1C.[Na+]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (107.19 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[3]

Human PPARδ, PPARα and PPARγ activity is monitored in transiently transfected cells treated with increasing concentrations of MBX-8025 (0.1 nM, 1 nM, 10 nM, 100, nM, 1000 nM) in comparison with reference compounds (0.1 nM-1 μM) for individual subtypes. The PPAR subtype selectivity of MBX-8025 is evaluated in a cell-based GAL4 reporter assay system[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

Mouse: From weaning (week 4), Alms1 mutant (foz/foz) NOD.B10 mice or Wt littermates (female mice in both groups) are fed an atherogenic diet (23% fat, 0.2% cholesterol and 45% simple carbohydrate; 4.78 kcal/g digestible energy) ad libitum for 16 weeks, after which groups are randomized (n=8 to 12 mice/group) to once-a-day oral administration (by gavage) for 8 weeks of Seladelpar sodium salt (10 mg/kg in 1% methylcellulose) or vehicle (controls). Animals are housed under 12-hour light/dark cycle and constant temperature of 22°C and receive maximal humane care[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

SeladelparMBX-8025RWJ-800025MBX8025MBX 8025RWJ800025RWJ 800025PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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Product name:
Seladelpar sodium salt
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HY-19522A
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