2. GPCR/G Protein
  3. GPR84
  4. GLPG1205

GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis. GLPG1205 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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GLPG1205 Chemical Structure

GLPG1205 Chemical Structure

CAS No. : 1445847-37-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 292 In-stock
Solution
10 mM * 1 mL in DMSO USD 292 In-stock
Solid
5 mg USD 265 In-stock
10 mg USD 450 In-stock
50 mg USD 1500 In-stock
100 mg USD 2800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

GLPG1205 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis[1][2]. GLPG1205 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Cellular Effect
Cell Line Type Value Description References
Neutrophil IC50
11 nM
Compound: (S)-36
Inhibition of embelin-induced migration of human neutrophils preincubated for 30 mins followed by embelin addition and measured after 1 hr by ATPlite luminescence assay
Inhibition of embelin-induced migration of human neutrophils preincubated for 30 mins followed by embelin addition and measured after 1 hr by ATPlite luminescence assay
[PMID: 32902984]
Neutrophil IC50
111 nM
Compound: (S)-36
Inhibition of embelin-induced migration of rat neutrophils preincubated for 30 mins followed by embelin addition and measured after 1 hr by celltiter-glo assay
Inhibition of embelin-induced migration of rat neutrophils preincubated for 30 mins followed by embelin addition and measured after 1 hr by celltiter-glo assay
[PMID: 32902984]
In Vitro

GLPG1205 (0.5?μM) completely inhibits the ZQ16-induced [Ca2+]i response in neutrophils[1].
? GLPG1205 (1?μM; for 5?min) completely blocks the ROS-response induced by the GPR84-agonist[1].
? GLPG1205 can potently antagonizes ZQ16-induced ROS with an IC50 value of 15?nM in TNF-α primed neutrophils[1].

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

GLPG1205 Related Antibodies
In Vivo

GLPG1250 (orally adminstation; 30mg/kg; twice daily) for 2 weeks, starts from 7 days post-challenge,greatly reduces the Ashcroft score, in idiopathic pulmonary fibrosis model[3].
? GLPG1250 (orally adminstation; 30mg/kg; once daily) starts from 18 weeks post irradition, significantly reduces college deposition in the mouse lung. Additionlly, GLPG1250 inhibits the increase in MnSOD in lung bronchial epithelial cells and parenchymal macrophages, in the irradiation model[3].
? GLPG1205 dose dependently decreases disease activity, histological activity, neutrophil influx and colonic MPO content,in a mouse IBD model[4].

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

378.42

Formula

C22H22N2O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N=C(OC[C@H]2OCCOC2)C=C3N1CCC4=C3C=CC(C#CC5CC5)=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 : 250 mg/mL (660.64 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 2.6426 mL 13.2128 mL 26.4257 mL
5 mM 0.5285 mL 2.6426 mL 5.2851 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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:  0.5% CMC-Na/1% Tween-80 in Saline water

    Solubility: 16.78 mg/mL (44.34 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 6.25 mg/mL (16.52 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 6.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  0.5% CMC-Na/saline water

    Solubility: 5 mg/mL (13.21 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
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, 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6426 mL 13.2128 mL 26.4257 mL 66.0642 mL
5 mM 0.5285 mL 2.6426 mL 5.2851 mL 13.2128 mL
10 mM 0.2643 mL 1.3213 mL 2.6426 mL 6.6064 mL
15 mM 0.1762 mL 0.8809 mL 1.7617 mL 4.4043 mL
20 mM 0.1321 mL 0.6606 mL 1.3213 mL 3.3032 mL
25 mM 0.1057 mL 0.5285 mL 1.0570 mL 2.6426 mL
30 mM 0.0881 mL 0.4404 mL 0.8809 mL 2.2021 mL
40 mM 0.0661 mL 0.3303 mL 0.6606 mL 1.6516 mL
50 mM 0.0529 mL 0.2643 mL 0.5285 mL 1.3213 mL
60 mM 0.0440 mL 0.2202 mL 0.4404 mL 1.1011 mL
80 mM 0.0330 mL 0.1652 mL 0.3303 mL 0.8258 mL
100 mM 0.0264 mL 0.1321 mL 0.2643 mL 0.6606 mL
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GLPG1205 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GLPG12051445847-37-9GLPG 1205GLPG-1205GPR84G protein coupled receptor 84G-protein-coupledreceptoractivationGTPγSbindingassayanti-inflammatoryactivitypulmonaryfibrosis， IBDInhibitorinhibitorinhibit

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