2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. GSK-4716

GSK-4716 is a selective ERRβ/γ agonist.

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GSK-4716

GSK-4716 構造式

CAS 番号 : 101574-65-6

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 53 在庫あり
Solution
10 mM * 1 mL in DMSO USD 53 在庫あり
Solid
5 mg $49 在庫あり
10 mg $79 在庫あり
25 mg $175 在庫あり
50 mg $280 在庫あり
100 mg $480 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 5 publication(s) in Google Scholar

GSK-4716 関連抗体

Top Publications Citing Use of Products

Estrogen Receptor/ERR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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  • プロトコル

  • 純度とドキュメンテーション

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製品説明

GSK-4716 is a selective ERRβ/γ agonist.

IC50 & Target

ERRβ/γ[1]
体外実験

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.

GSK-4716 関連抗体
分子量

282.34

分子式

C17H18N2O2
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.
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.
純度とドキュメンテーション

純度: 99.63%

COA (244 KB) HNMR (147 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
参考文献
細胞実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

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.

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
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GSK-4716 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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製品名:
GSK-4716
製品番号:
HY-33353
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