GPR84 antagonist 8

Name: GPR84 antagonist 8
Brand: MedChemExpress
SKU: HY-112562
Rating: 4.5 (2 reviews)

Cat. No.: HY-112562 Purity: 99.85%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GPR84 antagonist 8 is a selective GPR84 antagonist.

For research use only. We do not sell to patients.

GPR84 antagonist 8 Chemical Structure

CAS No. : 1445846-30-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 242	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 242	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 700	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1980	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE GPR84 antagonist 8

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

GPR84 antagonist 8 is a selective GPR84 antagonist.

IC₅₀ & Target

GPR84^[1]

In Vitro

GPR84 is a member of the metabolic G protein-coupled receptor family, and its expression has been described predominantly in immune cells. To test the hypothesis that blocking the activation of GPR84 can be a potential anti-inflammatory strategy in different inflammatory diseases, GPR84 antagonist 8 is used. The potency and specificity of GPR84 antagonist 8 is assessed tusing GPR84-CHO cells in the cAMP assay. GPR84 antagonist 8 effectively inhibits the action of 6-OAU in decreasing cAMP production in GPR84-CHO cells. To test GPR84 antagonist 8’s inhibition of the pro-inflammatory effects of GPR84 activation in macrophages, LPS pre-treated BMDMs are incubated with 10 µM GPR84 antagonist 8 for 30 min before adding 1 µM 6-OAU. Protein analysis by Western Blot shows that the GPR84 antagonist 8 partially blocks the phosphorylation of AKT and ERK induced by 6-OAU^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

421.45

Formula

C₂₃H₂₃N₃O₅

CAS No.

1445846-30-9

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1N=C(OCC2OCCOC2)C=C3N1CCC4=C3C=CC(OCC5=NC=CC=C5)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 5 mg/mL (11.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3728 mL	11.8638 mL	23.7276 mL
5 mM	0.4746 mL	2.3728 mL	4.7455 mL
10 mM	0.2373 mL	1.1864 mL	2.3728 mL

View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.54 mg/mL (1.28 mM); Clear solution

This protocol yields a clear solution of ≥ 0.54 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.4 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.54 mg/mL (1.28 mM); Clear solution

This protocol yields a clear solution of ≥ 0.54 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.4 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.54 mg/mL (1.28 mM); Clear solution

This protocol yields a clear solution of ≥ 0.54 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.4 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.85%

Select Batch:

Data Sheet (273 KB) SDS (0 KB)

COA (246 KB) LCMS (269 KB)

Handling Instructions (2659 KB)

References

[1]. Recio C, et al. Activation of the Immune-Metabolic Receptor GPR84 Enhances Inflammation and Phagocytosis in Macrophages. Front Immunol. 2018 Jun 20;9:1419. [Content Brief]

Cell Assay
^[1]

Bone marrow-derived macrophages treated with either vehicle (0.3% DMSO) or 1 µM 6-OAU for 1 h are incubated with unopsonised pHrodo E. coli bioparticles at 0.1 mg/mL in a 96-well flat clear bottom plate. For the inhibition studies with GPR84 antagonist 8, cells are pretreated with 10 µM GPR84 antagonist 8 for 30 min before addition of either vehicle or 6-OAU. The plate is then placed into the IncuCyte Zoom platform which is housed inside a humidified incubator at 37°C, 5% CO₂. Two to four images per well from three technical replicates are taken every 15 min for 4 h^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Recio C, et al. Activation of the Immune-Metabolic Receptor GPR84 Enhances Inflammation and Phagocytosis in Macrophages. Front Immunol. 2018 Jun 20;9:1419. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3728 mL	11.8638 mL	23.7276 mL	59.3190 mL
	5 mM	0.4746 mL	2.3728 mL	4.7455 mL	11.8638 mL
	10 mM	0.2373 mL	1.1864 mL	2.3728 mL	5.9319 mL