GPR84 antagonist 3
Based on 1 publication(s) in Google Scholar
GPR84 antagonist 3 (compound 42) is a potent GPR84 (G-protein-coupled receptor 84) antagonist. GPR84 antagonist 3 inhibits GTPγS, with a pIC50 of 8.28. GPR84 antagonist 3 has a favorable pharmacokinetic profile suitable.
For research use only. We do not sell to patients.
- Purity: 98.32%
- CAS No.: 2815263-05-7
- Formula: C29H27N5O
- Molecular Weight:461.56
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GPR84 antagonist 3
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Biological Activity
pIC50: 8.28 ± 0.11 (GTPγS)[1]
GPR84 antagonist 3 (compound 42) displays no ability to block the actions of the C3 fatty acid propionate at either FFAR2 or FFAR3 when tested at 10 μM[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (n = 3)[1]
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Dosage:1 mg/kg (IV), 10 mg/kg (Orally)
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Administration:IV, Orally; once (Pharmacokinetic Analysis)
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Result:Pharmacokinetic Parameters of GPR84 antagonist 3 in Male C57BL/6J mice[1].
IV (1 mg/kg) PO (10 mg/kg) half-life (h) 2.51 ± 6.55 CL (mL/min/kg) 38.9 ± 13.9 Vss (L/kg) 7.24 ± 9.2 C0 (ng/mL) 394 ± 19.1 AUCall (ng/mL·h) 420 ± 12.5 1590 ± 18.7 Tmax (h) 1 Cmax (ng/mL) 402 ± 31.8 F (%) 36.8 ± 18.7
Chemical Information
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CAS No. 2815263-05-7
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Appearance Solid
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Molecular Weight 461.56
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Formula C29H27N5O
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Color Light yellow to yellow
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SMILES
N1(CC2=CC=C(C3=C(C4=CC=CC=C4)N=C(CC5=CNC6=C5C=CC=C6)N=N3)C=C2)CCOCC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Brain Behav
G-Protein-Coupled Receptor 84 Aggravates Early Brain Injury via Microglial NLRP3-ASC Inflammasome After Subarachnoid Hemorrhage. [Abstract]2025 Apr;15(4):e70379. PMID: 40200750
Solvent & Solubility
DMSO : 100 mg/mL (216.66 mM; Need ultrasonic; 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 (5.42 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.
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.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 2.1666 mL | 10.8328 mL | 21.6657 mL | 54.1641 mL |
| 5 mM | 0.4333 mL | 2.1666 mL | 4.3331 mL | 10.8328 mL | |
| 10 mM | 0.2167 mL | 1.0833 mL | 2.1666 mL | 5.4164 mL | |
| 15 mM | 0.1444 mL | 0.7222 mL | 1.4444 mL | 3.6109 mL | |
| 20 mM | 0.1083 mL | 0.5416 mL | 1.0833 mL | 2.7082 mL | |
| 25 mM | 0.0867 mL | 0.4333 mL | 0.8666 mL | 2.1666 mL | |
| 30 mM | 0.0722 mL | 0.3611 mL | 0.7222 mL | 1.8055 mL | |
| 40 mM | 0.0542 mL | 0.2708 mL | 0.5416 mL | 1.3541 mL | |
| 50 mM | 0.0433 mL | 0.2167 mL | 0.4333 mL | 1.0833 mL | |
| 60 mM | 0.0361 mL | 0.1805 mL | 0.3611 mL | 0.9027 mL | |
| 80 mM | 0.0271 mL | 0.1354 mL | 0.2708 mL | 0.6771 mL | |
| 100 mM | 0.0217 mL | 0.1083 mL | 0.2167 mL | 0.5416 mL |
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