Art. -Nr.: HY-111254

GQ-16

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GQ-16 is an orally active PPARγ partial agonist with an IC₅₀ of 1.84 μM and a K_i of 160 nM against human PPARγ. GQ-16 inhibits Cdk5-mediated Ser-273 phosphorylation. GQ-16 improves insulin sensitivity and glucose tolerance in obese and diabetic mice. GQ-16 also exhibits certain cytotoxicity against tumor cells. GQ-16 can be used in research related to obesity, diabetes and cancer.

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Reinheit: 98.12%
CAS. Nr.: 870554-67-9
Formel: C₁₉H₁₆BrNO₃S
Molecular Weight:418.30

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

GQ-16 Chemical Structure

CAS. Nr.: 870554-67-9

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle PPAR Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Alle JNK Isoform-spezifische Produkte anzeigen :

In Vitro

GQ-16 (7 days) promotes the differentiation of 3T3-L1 preadipocytes and upregulates the expression of adipogenic genes, but its efficacy is lower than that of Rosiglitazone (HY-17386)^[1].
GQ-16 (10 nM-10 μM; 24 h) weakly activates the expression of PPARγ target genes acca1b and fgf21, and inhibits the expression of vcam1 and dcn in mature 3T3-L1 adipocytes^[1].
GQ-16 (10 μM; 6-48 h) weakly and transiently upregulates the expression of OLR1 in mature 3T3-L1 adipocytes, with its activity peak occurring at 10 h post-treatment^[1].
GQ-16 (10 μM; 4 days) exhibits reduced adipogenic potential in C3H10T1/2 and NIH-3T3L1 cells, with less intracellular lipid accumulation and lower aP2 expression levels compared to Rosiglitazone (HY-17386)^[2].
GQ-16 (10 nM-100 μM; 24-48 h) reduces the viability of MCF-7 cells^[3].

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

Real Time qPCR^[1]

Cell Line:

Mature 3T3-L1 adipocytes
Concentration:

0.01, 0.1, 1, 10 μM
Incubation Time:

24 h
Result:

Dose-dependently increased expression of acca1b and fgf21.
Dose-dependently repressed expression of vcam1 and dcn.

In Vivo

GQ-16 (20 mg/kg; p.o.; 10-15 days) improves insulin sensitivity and glucose tolerance in mice with diet-induced insulin resistance^[2].

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

Animal Model:

Swiss mice (male, 12 weeks old, fed high fat diet from 4 weeks of age)^[2]
Dosage:

20 mg/kg/day
Administration:

oral gavage; daily; 10, 12, or 15 days (depending on endpoint)
Result:

Reversed high fat diet-mediated impairments in insulin signaling, including increased phosphorylation of the insulin receptor, insulin receptor substrate 1, and protein kinase B in adipose tissue, liver, and muscle.
Reversed high fat diet-dependent suppression of inhibitor of nuclear factor κB (IκBα) protein and reduced high fat diet-dependent phosphorylation of JNK in adipose tissue, liver, and muscle.
Increased the plasma glucose disappearance rate (Kitt) to improve insulin sensitivity.
Improved glucose tolerance.
Did not elicit increased weight gain relative to high fat diet-fed controls.

Chemical Information

CAS. Nr. 870554-67-9
Appearance Solid
Molecular Weight 418.30
Formel C₁₉H₁₆BrNO₃S
Color Off-white to light yellow
SMILES

O=C(N(CC1=CC=C(C)C=C1)C/2=O)SC2=C/C3=CC(Br)=CC=C3OC
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 10 mg/mL (23.91 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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3906 mL

11.9531 mL

23.9063 mL

5 mM

0.4781 mL

2.3906 mL

4.7813 mL

10 mM

0.2391 mL

1.1953 mL

2.3906 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 90% Corn Oil

Solubility: ≥ 1 mg/mL (2.39 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ferreira A P B, et al. Effect of PPAR Partial Agonist, GQ‐16, on Viability of Breast Cancer Cells in Culture. The FASEB Journal, 2017, 31: 876.5-876.5.

[2]. Milton FA, et al. PPARγ partial agonist GQ-16 strongly represses a subset of genes in 3T3-L1 adipocytes. Biochem Biophys Res Commun. 2015 Aug 28;464(3):718-23. [Content Brief]

[3]. Amato AA, et al. GQ-16, a novel peroxisome proliferator-activated receptor γ (PPARγ) ligand, promotes insulin sensitization without weight gain. J Biol Chem. 2012;287(33):28169-28179. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.3906 mL	11.9531 mL	23.9063 mL	59.7657 mL
	5 mM	0.4781 mL	2.3906 mL	4.7813 mL	11.9531 mL
	10 mM	0.2391 mL	1.1953 mL	2.3906 mL	5.9766 mL
	15 mM	0.1594 mL	0.7969 mL	1.5938 mL	3.9844 mL
	20 mM	0.1195 mL	0.5977 mL	1.1953 mL	2.9883 mL

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GQ-16

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Alle PPAR Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Alle JNK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GQ-16 Related Classifications

HY-111254 Related Classifications