GQ-16
Based on 1 Customer Validation
GQ-16 is an orally active PPARγ partial agonist with an IC50 of 1.84 μM and a Ki 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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- Pureté: 98.12%
- CAS No.: 870554-67-9
- Formule: C19H16BrNO3S
- Masse moléculaire:418.30
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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.
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Cell Line:Mature 3T3-L1 adipocytes
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Concentration:0.01, 0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Dose-dependently increased expression of acca1b and fgf21.
Dose-dependently repressed expression of vcam1 and dcn.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss mice (male, 12 weeks old, fed high fat diet from 4 weeks of age)[2]
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Dosage:20 mg/kg/day
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Administration:oral gavage; daily; 10, 12, or 15 days (depending on endpoint)
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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
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CAS No. 870554-67-9
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Appearance Solid
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Masse moléculaire 418.30
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Formule C19H16BrNO3S
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Color Off-white to light yellow
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SMILES
O=C(N(CC1=CC=C(C)C=C1)C/2=O)SC2=C/C3=CC(Br)=CC=C3OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (278 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[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]
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 | 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 |
GQ-16 Related Classifications
HY-111254 Related Classifications
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