| Size | Price | Stock | Qty |
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| 5mg |
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| 50mg |
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| Targets |
ZQ-16 specifically targets GPR84, a G protein-coupled receptor that is activated by medium-chain fatty acids and plays a role in immune function and inflammation. It acts as a potent and selective agonist, activating the receptor with an EC50 of 139 nM (0.213 μM). It activates multiple downstream signaling pathways, including calcium mobilization, inhibition of cAMP accumulation, and ERK1/2 phosphorylation.
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| ln Vitro |
ZQ-16 has an EC50 value of 0.213 μM and causes dose-dependent calcium responses [1]. Moreover, ZQ-16 reduced forskolin-stimulated cAMP buildup in GPR84-expressing HEK293 cells in a dose-dependent manner, with an EC50 value of 0.134 μM [1]. In HEK293 cells expressing GPR84, ZQ-16 (10 μM; 5 min) also causes phosphorylation of ERK1/2 [1]. ZQ-16 causes β-arrestin2 recruitment, internalization, and desensitization of GPR84. With an EC50 value of 0.597 μM, ZQ-16 causes dose-dependent recruitment of β-Arrestin2 to GPR84 in HEK293 cells expressing both proteins [1].
In vitro, ZQ-16 is a potent and selective agonist for GPR84. It activates several GPR84-mediated signaling pathways, including calcium mobilization, inhibition of cAMP accumulation, phosphorylation of ERK1/2, receptor desensitization and internalization, and receptor-β-arrestin interaction. Its EC50 of 0.213 μM demonstrates its high potency. |
| ln Vivo |
In vivo activity data for ZQ-16 are not extensively detailed. As a potent and selective GPR84 agonist, it is a valuable tool for studying the role of this receptor in inflammation and immune function. It is used in animal models to investigate the effects of GPR84 activation, but specific protocols are not mentioned in the search results.
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| Enzyme Assay |
For non-cellular in vitro receptor binding assays, ZQ-16 is characterized using radioligand binding or other biophysical techniques to confirm its affinity and selectivity for GPR84. Its selectivity is validated by showing no activity at other FFARs at high concentrations (100 μM).
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HEK293 cells Tested Concentrations: 10 μM Incubation Duration: 5 min Experimental Results: Induced phosphorylation of ERK1/2. For in vitro cellular assays, the activity of ZQ-16 is evaluated in cells expressing GPR84. Key functional assays include measuring the mobilization of intracellular calcium, the inhibition of cAMP accumulation, and the phosphorylation of ERK1/2. These assays confirm its agonistic activity and are used to study the receptor's pharmacology and signaling. |
| Animal Protocol |
In vivo animal studies with ZQ-16 would typically be conducted in mouse models to investigate the role of GPR84 in inflammation and immune function. For example, it could be used in models of colitis, sepsis, or other inflammatory diseases. The compound can be administered via various routes, including oral or intraperitoneal injection, depending on the study design.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for ZQ-16 are not extensively documented. As a small-molecule agonist, it is expected to have moderate oral bioavailability. Information concerning product stability, particularly in solution, has rarely been reported. Its solubility and formulation for in vivo studies would need to be determined empirically.
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| Toxicity/Toxicokinetics |
Toxicological data for ZQ-16 are limited. As a research compound, it is intended for laboratory use only and not for human therapeutic applications. Its safety profile has not been established for clinical use. At the concentrations used in research, it is generally considered to have low toxicity, but standard laboratory safety practices should always be followed.
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| References | |
| Additional Infomation |
GPR84 agonist; structure can be found in the first article.
ZQ-16 is a potent and selective agonist for the medium-chain free fatty acid receptor GPR84, with an EC50 of 139 nM (0.213 μM). It activates multiple downstream signaling pathways and shows no activity at GPR40, GPR41, GPR119, or GPR120 at 100 μM. It is a key research tool for studying GPR84 function. |
| Molecular Formula |
C10H16N2O2S
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|---|---|
| Molecular Weight |
228.31
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| Exact Mass |
228.093
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| CAS # |
376616-73-8
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| PubChem CID |
1912564
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.588
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| LogP |
2.68
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
15
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| Complexity |
287
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCSC1=NC(=CC(=O)N1)O
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| InChi Key |
UYXOAKRMLQKLQX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H16N2O2S/c1-2-3-4-5-6-15-10-11-8(13)7-9(14)12-10/h7H,2-6H2,1H3,(H2,11,12,13,14)
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| Chemical Name |
2-hexylsulfanyl-4-hydroxy-1H-pyrimidin-6-one
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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: 25 mg/mL (109.50 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3800 mL | 21.9000 mL | 43.8001 mL | |
| 5 mM | 0.8760 mL | 4.3800 mL | 8.7600 mL | |
| 10 mM | 0.4380 mL | 2.1900 mL | 4.3800 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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