2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. DS45500853

DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).

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DS45500853 Chemical Structure

DS45500853 Chemical Structure

CAS No. : 2735803-28-6

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

DS45500853 Related Antibodies

Top Publications Citing Use of Products

View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • Biological Activity

  • Purity & Documentation

  • References

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Description

DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM)[1].

IC50 & Target[1]

ERRα

 

In Vitro

DS45500853 (compound 5c; 0.002, 0.006, 0.017, 0.051, 0.015, 0.046, 1.4, 4.2, 12.5 μg/mL; 18 h) activates the transcriptional activity of full-length ERRα in MG63 cells with an EC50 of 5.4 μM[1].
DS45500853 binds in the ligand-binding pocket (LBP) of the ERRα LBD as inverse agonist II[1].

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

DS45500853 Related Antibodies
Molecular Weight

284.35

Formula

C18H20O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C1=CC=C(OC2=CC=C(O)C(C(C)(C)C)=C2)C=C1)=O
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 (175.84 mM; ultrasonic and warming and heat to 60°C; 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 3.5168 mL 17.5840 mL 35.1679 mL
5 mM 0.7034 mL 3.5168 mL 7.0336 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. 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
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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: ≥ 0.5 mg/mL (1.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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: ≥ 0.5 mg/mL (1.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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).
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
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. 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 3.5168 mL 17.5840 mL 35.1679 mL 87.9198 mL
5 mM 0.7034 mL 3.5168 mL 7.0336 mL 17.5840 mL
10 mM 0.3517 mL 1.7584 mL 3.5168 mL 8.7920 mL
15 mM 0.2345 mL 1.1723 mL 2.3445 mL 5.8613 mL
20 mM 0.1758 mL 0.8792 mL 1.7584 mL 4.3960 mL
25 mM 0.1407 mL 0.7034 mL 1.4067 mL 3.5168 mL
30 mM 0.1172 mL 0.5861 mL 1.1723 mL 2.9307 mL
40 mM 0.0879 mL 0.4396 mL 0.8792 mL 2.1980 mL
50 mM 0.0703 mL 0.3517 mL 0.7034 mL 1.7584 mL
60 mM 0.0586 mL 0.2931 mL 0.5861 mL 1.4653 mL
80 mM 0.0440 mL 0.2198 mL 0.4396 mL 1.0990 mL
100 mM 0.0352 mL 0.1758 mL 0.3517 mL 0.8792 mL
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DS45500853 Related Classifications

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.

Keywords:

DS455008532735803-28-6DS 45500853DS-45500853Estrogen Receptor/ERRRIP140metabolic disordersT2DMMG63 cellstranscriptional activityInhibitorinhibitorinhibit

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