ZQ-16
Based on 1 Customer Validation
ZQ-16 is a potent and selective GPR84 agonist with an EC50 value of 0.213 μM. ZQ-16 has no activity on the other free fatty acid receptors (FFARs), including GPR40, GPR41, GPR119 and GPR120.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.0%
- No. CAS: 376616-73-8
- Fòrmula: C10H16N2O2S
- Peso molecular:228.31
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.134 μM
Compound: 4
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Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF as
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF as
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[PMID: 31721581] |
| HEK293 | EC50 |
0.139 μM
Compound: 1
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Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
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[PMID: 27326330] |
| HEK293 | EC50 |
0.213 μM
Compound: 4
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Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay
Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay
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[PMID: 31721581] |
| HEK293 | EC50 |
0.597 μM
Compound: 4
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Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay
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[PMID: 31721581] |
| HEK293 | EC50 |
144 nM
Compound: 1
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Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
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[PMID: 27326330] |
ZQ-16 induces calcium response in a dose-dependent manner, with an EC50 value of 0.213 μM[1].
ZQ-16 also induces dose-dependent reduction of Forskolin-stimulated cAMP accumulation in HEK293 cells expressing GPR84 with an EC50 value of 0.134 μM[1].
ZQ-16 (10 μM; 5 min) also induces phosphorylation of ERK1/2 in GPR84-expressing HEK293 cells[1].
ZQ-16 induces GPR84 desensitization, internalization, and β-arrestin2 recruitment. ZQ-16 induced a dose-dependent recruitment of β-Arrestin2 towards GPR84 in HEK293 cells expressing both proteins with an EC50 value of 0.597 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:10 μM
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Incubation Time:5 min
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Result:Induced phosphorylation of ERK1/2.
Chemical Information
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No. CAS 376616-73-8
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Appearance Solid
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Peso molecular 228.31
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Fòrmula C10H16N2O2S
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Color White to off-white
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SMILES
O=C1NC(SCCCCCC)=NC(O)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 25 mg/mL (109.50 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.95 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.95 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.
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.
Pureza y Documentación
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Ficha de datos (271 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 4.3800 mL | 21.9000 mL | 43.8001 mL | 109.5002 mL |
| 5 mM | 0.8760 mL | 4.3800 mL | 8.7600 mL | 21.9000 mL | |
| 10 mM | 0.4380 mL | 2.1900 mL | 4.3800 mL | 10.9500 mL | |
| 15 mM | 0.2920 mL | 1.4600 mL | 2.9200 mL | 7.3000 mL | |
| 20 mM | 0.2190 mL | 1.0950 mL | 2.1900 mL | 5.4750 mL | |
| 25 mM | 0.1752 mL | 0.8760 mL | 1.7520 mL | 4.3800 mL | |
| 30 mM | 0.1460 mL | 0.7300 mL | 1.4600 mL | 3.6500 mL | |
| 40 mM | 0.1095 mL | 0.5475 mL | 1.0950 mL | 2.7375 mL | |
| 50 mM | 0.0876 mL | 0.4380 mL | 0.8760 mL | 2.1900 mL | |
| 60 mM | 0.0730 mL | 0.3650 mL | 0.7300 mL | 1.8250 mL | |
| 80 mM | 0.0548 mL | 0.2738 mL | 0.5475 mL | 1.3688 mL | |
| 100 mM | 0.0438 mL | 0.2190 mL | 0.4380 mL | 1.0950 mL |
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