GPR84 antagonist 3

Name: GPR84 antagonist 3
Brand: MedChemExpress
SKU: HY-151100
Rating: 4.5 (1 reviews)

Cat. No.: HY-151100 Purity: 99.54%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

GPR84 antagonist 3 Chemical Structure

CAS No. : 2815263-05-7

Size	Price	Stock	Quantity
5 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2250	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

pIC50: 8.28 ± 0.11 (GTPγS)^[1]

In Vitro

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.

In Vivo

GPR84 antagonist 3 (compound 42) (1 mg/kg (IV), 10 mg/kg (Orally); once) has a good elimination half-life (2.51 h), moderate rate of clearance, and bioavailability^[1].

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

Animal Model:

Male C57BL/6J mice (n = 3)^[1]

Dosage:

1 mg/kg (IV), 10 mg/kg (Orally)

Administration:

IV, Orally; once (Pharmacokinetic Analysis)

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
T_max (h)		1
C_max (ng/mL)		402 ± 31.8
F (%)		36.8 ± 18.7

Molecular Weight

461.56

Formula

C₂₉H₂₇N₅O

CAS No.

2815263-05-7

Appearance

Solid

Color

Light yellow to yellow

SMILES

N1(CC2=CC=C(C3=C(C4=CC=CC=C4)N=C(CC5=CNC6=C5C=CC=C6)N=N3)C=C2)CCOCC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1666 mL	10.8328 mL	21.6657 mL
5 mM	0.4333 mL	2.1666 mL	4.3331 mL
10 mM	0.2167 mL	1.0833 mL	2.1666 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, 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.

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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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 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.

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: 99.54%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (252 KB) HNMR (274 KB) LCMS (101 KB)

Handling Instructions (2659 KB)

References

[1]. Mahindra A, et al. Investigating the Structure-Activity Relationship of 1,2,4-Triazine G-Protein-Coupled Receptor 84 (GPR84) Antagonists. J Med Chem. 2022 Aug 10. [Content Brief]

Complete Stock Solution Preparation Table

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