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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: 98.77%
COA 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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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 150 In-stock
50 mg USD 490 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

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  • References

  • Customer Review

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

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].

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

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].

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

Clinical Trial
Molecular Weight

466.45

Formula

C21H22F3NaO5S

Appearance

Solid

Color

White to off-white

SMILES

O=C(O[Na])COC1=CC=C(SC[C@H](OCC)COC2=CC=C(C(F)(F)F)C=C2)C=C1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (107.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.77%

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1439 mL 10.7193 mL 21.4385 mL 53.5963 mL
5 mM 0.4288 mL 2.1439 mL 4.2877 mL 10.7193 mL
10 mM 0.2144 mL 1.0719 mL 2.1439 mL 5.3596 mL
15 mM 0.1429 mL 0.7146 mL 1.4292 mL 3.5731 mL
20 mM 0.1072 mL 0.5360 mL 1.0719 mL 2.6798 mL
25 mM 0.0858 mL 0.4288 mL 0.8575 mL 2.1439 mL
30 mM 0.0715 mL 0.3573 mL 0.7146 mL 1.7865 mL
40 mM 0.0536 mL 0.2680 mL 0.5360 mL 1.3399 mL
50 mM 0.0429 mL 0.2144 mL 0.4288 mL 1.0719 mL
60 mM 0.0357 mL 0.1787 mL 0.3573 mL 0.8933 mL
80 mM 0.0268 mL 0.1340 mL 0.2680 mL 0.6700 mL
100 mM 0.0214 mL 0.1072 mL 0.2144 mL 0.5360 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Seladelpar sodium salt
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HY-19522A
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