GSK-4716

Name: GSK-4716
Brand: MedChemExpress
SKU: HY-33353
Rating: 5.0 (4 reviews)

Cat. No.: HY-33353 Purity: 99.82%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GSK-4716 is a selective ERRβ/γ agonist.

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

GSK-4716 Chemical Structure

CAS No. : 101574-65-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 53	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 53	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 49	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 79	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 194	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 343	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 607	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE GSK-4716

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View All Isoforms

Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

GSK-4716 is a selective ERRβ/γ agonist.

IC₅₀ & Target

ERRβ/γ^[1]

In Vitro

Treatment of differentiated C2C12 cells with the ERRβ/γ agonist (relative to vehicle) over a 2 to 4 h time period reveals a reproducible and robust increase in the immunoreactivity of the GRα-D isoform. It is observed that MAO-A mRNA expression is significantly increased by treatment with the ERRβ/γ agonist, GSK4716. Furthermore, it is observed that GSK4716 induces the expression of the mRNAs encoding peroxisome proliferator-activated receptor-γcoactivator 1α (PGC-1α) and PGC-1β (key regulator of many metabolic genes) identified as direct coactivators for the ERR family. GSK4716 induces the expression of PGC-1 and genes involved in fatty acid oxidation in concordance with the characterized role of ERRγ in cardiac metabolism^[1]. Treatment of primary mouse myotubes with GSK4716, an ERRβ/γ agonist, results in a concerted increase in the expression levels of Ppargc1a, Ppargc1b, and the Esrr genes. Furthermore,Cpt1b, Atp5b, and Idh3, genes in key mitochondrial pathways, are also induced by GSK4716. Additionally, GSK4716 increases citrate synthase activity and cytochrome c protein levels^[2].

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

Molecular Weight

282.34

Formula

C₁₇H₁₈N₂O₂

CAS No.

101574-65-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(N/N=C/C1=CC=C(C(C)C)C=C1)C2=CC=C(O)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (354.18 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.5418 mL	17.7091 mL	35.4183 mL
5 mM	0.7084 mL	3.5418 mL	7.0837 mL
10 mM	0.3542 mL	1.7709 mL	3.5418 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (8.85 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 (8.85 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.82%

Select Batch:

Data Sheet (273 KB) SDS (537 KB)

COA (244 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

References

[1]. Wang SC, et al. An ERRbeta/gamma agonist modulates GRalpha expression, and glucocorticoid responsive gene expression in skeletal muscle cells. Mol Cell Endocrinol. 2010 Feb 5;315(1-2):146-52. [Content Brief]

[2]. Rangwala SM, et al. Estrogen-related receptor gamma is a key regulator of muscle mitochondrial activity and oxidative capacity. J Biol Chem. 2010 Jul 16;285(29):22619-29. [Content Brief]

Cell Assay
^[1]

Proliferating mouse C2C12 myoblast are cultured and maintained in DMEM supplemented with 10% heat-inactivated serum supreme. Differentiation of myoblasts into post-mitotic, multi-nucleated myotubes are induced by mitogen withdrawal (DMEM supplemented with 2% horse serum) for 4 days. C2C12 myotubes are treated with either vehicle (DMSO) or ERRβ/γ agonist GSK4716 for 1 day and RNA collected and processed^[1].

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

References

[1]. Wang SC, et al. An ERRbeta/gamma agonist modulates GRalpha expression, and glucocorticoid responsive gene expression in skeletal muscle cells. Mol Cell Endocrinol. 2010 Feb 5;315(1-2):146-52. [Content Brief]

[2]. Rangwala SM, et al. Estrogen-related receptor gamma is a key regulator of muscle mitochondrial activity and oxidative capacity. J Biol Chem. 2010 Jul 16;285(29):22619-29. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.5418 mL	17.7091 mL	35.4183 mL	88.5457 mL
	5 mM	0.7084 mL	3.5418 mL	7.0837 mL	17.7091 mL
	10 mM	0.3542 mL	1.7709 mL	3.5418 mL	8.8546 mL
	15 mM	0.2361 mL	1.1806 mL	2.3612 mL	5.9030 mL
	20 mM	0.1771 mL	0.8855 mL	1.7709 mL	4.4273 mL
	25 mM	0.1417 mL	0.7084 mL	1.4167 mL	3.5418 mL
	30 mM	0.1181 mL	0.5903 mL	1.1806 mL	2.9515 mL
	40 mM	0.0885 mL	0.4427 mL	0.8855 mL	2.2136 mL
	50 mM	0.0708 mL	0.3542 mL	0.7084 mL	1.7709 mL
	60 mM	0.0590 mL	0.2952 mL	0.5903 mL	1.4758 mL
	80 mM	0.0443 mL	0.2214 mL	0.4427 mL	1.1068 mL
	100 mM	0.0354 mL	0.1771 mL	0.3542 mL	0.8855 mL

GSK-4716 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:

GSK-4716101574-65-6GSK4716GSK 4716Estrogen Receptor/ERRInhibitorinhibitorinhibit

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GSK-4716

Customer Review

GSK-4716 Related Antibodies

4 Publications Citing Use of MCE GSK-4716

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Estrogen Receptor/ERR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

GSK-4716 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GSK-4716 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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