| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| ln Vitro |
In vitro, GQ-16 binds to PPARγ with a Ki of 160 nM. It inhibits Cdk5-mediated Ser-273 phosphorylation. It acts as a partial agonist, reducing adipogenesis. It is specific for PPARγ and possesses no detectable activity for PPARα or PPARβ/δ.
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|---|---|
| ln Vivo |
In vivo, GQ-16 enhances insulin sensitivity and glucose tolerance in obese and diabetic mouse models. It promotes insulin sensitization without weight gain. It is an orally active compound.
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| Enzyme Assay |
In vitro assays for GQ-16 typically measure its binding to PPARγ. Radioligand binding assays are used to determine Ki values. Reporter gene assays using PPARγ-responsive luciferase constructs are used to assess its agonistic activity. Its ability to inhibit Cdk5-mediated phosphorylation is assessed by Western blotting using phospho-specific antibodies.
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| Cell Assay |
Cellular assays for GQ-16 are performed using adipocytes or other cell types expressing PPARγ. Cells are treated with the compound, and PPARγ target gene expression is measured by qRT-PCR. Adipogenesis is assessed by Oil Red O staining. Insulin sensitivity is assessed by measuring glucose uptake.
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| Animal Protocol |
In vivo animal studies with GQ-16 are conducted in obese and diabetic mouse models. The compound is administered orally. Glucose tolerance tests and insulin tolerance tests are performed. Body weight and adiposity are measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GQ-16 are limited. Its molecular weight is 418.30 g/mol. The compound is orally active. For research use, it is typically dissolved in DMSO for in vitro studies. Its half-life and metabolic profile have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for GQ-16 are limited. In animal studies, the compound promotes insulin sensitization without weight gain. No significant toxicity has been reported at the doses used for efficacy studies. The compound is intended for research use and should be handled with standard safety precautions.
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| References | |
| Additional Infomation |
GQ-16 is a research compound used as a partial agonist of PPARγ. It promotes insulin sensitization without weight gain. The compound is a valuable tool for studying PPARγ signaling and insulin resistance. It is not approved for clinical use and is intended for laboratory research only.
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| Molecular Formula |
C19H16BRNO3S
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|---|---|
| Molecular Weight |
418.305
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| Exact Mass |
417.003
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| CAS # |
870554-67-9
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| PubChem CID |
11509958
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
549.8±60.0 °C at 760 mmHg
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| Flash Point |
286.3±32.9 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.688
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| LogP |
5.79
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
545
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=CC=C(C=C1)CN2C(=O)/C(=C/C3=C(C=CC(=C3)Br)OC)/SC2=O
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| InChi Key |
AMLZLORVKZAHOH-YVLHZVERSA-N
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| InChi Code |
InChI=1S/C19H16BrNO3S/c1-12-3-5-13(6-4-12)11-21-18(22)17(25-19(21)23)10-14-9-15(20)7-8-16(14)24-2/h3-10H,11H2,1-2H3/b17-10-
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| Chemical Name |
(5Z)-5-[(5-bromo-2-methoxyphenyl)methylidene]-3-[(4-methylphenyl)methyl]-1,3-thiazolidine-2,4-dione
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| Synonyms |
GQ16 GQ 16 GQ-16
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~23.91 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3906 mL | 11.9529 mL | 23.9057 mL | |
| 5 mM | 0.4781 mL | 2.3906 mL | 4.7811 mL | |
| 10 mM | 0.2391 mL | 1.1953 mL | 2.3906 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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