2. Immunology/Inflammation
  3. IRAK
  4. GLPG2534

GLPG2534 is an orally active and selective IRAK4 inhibitor, with IC50 values of 6.4 nM and 3.5 nM for human and mouse IRAK4. GLPG2534 can be used for the research of inflammatory skin diseases.

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

GLPG2534 Chemical Structure

GLPG2534 Chemical Structure

CAS No. : 2095615-97-5

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5 mg USD 340 In-stock
10 mg USD 550 In-stock
25 mg USD 1090 In-stock
50 mg USD 1750 In-stock
100 mg USD 2800 In-stock
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Based on 1 publication(s) in Google Scholar

GLPG2534 Related Antibodies

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IRAK1 IRAK4

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  • Purity & Documentation

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Description

GLPG2534 is an orally active and selective IRAK4 inhibitor, with IC50 values of 6.4 nM and 3.5 nM for human and mouse IRAK4. GLPG2534 can be used for the research of inflammatory skin diseases[1].

IC50 & Target[1]

hIRAK4

6.4 nM (IC50)

mIRAK4

3.5 nM (IC50)

IRAK1

179 nM (IC50)

In Vitro

GLPG2534 (2 h) inhibits IRAK4 with IC50 values of 6.4 nM and 3.5 nM for human and mouse IRAK4[1].
GLPG2534 inhibits IL-1β–driven IL-6 release, with an IC50 of 55 nM[1].
GLPG2534 inhibits TNF-α–driven IL-6 release with an IC50 of 6.6 μM[1].
GLPG2534 (0.1-10 μM, 16 h) inhibits expression of S100A7, DEFB4A, CXCL8, TNF in Flagellin-stimulated keratinocytes[1].

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

GLPG2534 Related Antibodies
In Vivo

GLPG2534 (0.3-10 mg/kg, p.o.) Inhibits CL097-driven release of TNF-α in blood of mice[1].
GLPG2534 (10 and 30 mg/kg, p.o., b.i.d. 5 days) attenuates inflammation in psoriasis-like mouse models[1].
GLPG2534 (3-30 mg/kg, p.o., b.i.d. 5 days) attenuates the development of IL-33- and MC903-induced AD-like skin inflammation in mice[1].

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

Animal Model: Psoriasis-like skin inflammation model, induced by IL-23 and IMQ[1]
Dosage: 10 and 30 mg/kg
Administration: p.o., b.i.d. 5 days
Result: Reduced IL-23-induced expression of pathogenic cytokines such as Il17a (79%), Il22 (49%), Il1b (97%), and defensin Lcn2 (69%).
Molecular Weight

424.45

Formula

C21H24N6O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

N#CC(C=N1)=CC=C1N2C3=NC(NC4CCOCC4)=C(OCCOCCO)C=C3N=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (235.60 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 2.3560 mL 11.7800 mL 23.5599 mL
5 mM 0.4712 mL 2.3560 mL 4.7120 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.

  • 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:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.89 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (5.89 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. 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 (25.0 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)

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, 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 2.3560 mL 11.7800 mL 23.5599 mL 58.8998 mL
5 mM 0.4712 mL 2.3560 mL 4.7120 mL 11.7800 mL
10 mM 0.2356 mL 1.1780 mL 2.3560 mL 5.8900 mL
15 mM 0.1571 mL 0.7853 mL 1.5707 mL 3.9267 mL
20 mM 0.1178 mL 0.5890 mL 1.1780 mL 2.9450 mL
25 mM 0.0942 mL 0.4712 mL 0.9424 mL 2.3560 mL
30 mM 0.0785 mL 0.3927 mL 0.7853 mL 1.9633 mL
40 mM 0.0589 mL 0.2945 mL 0.5890 mL 1.4725 mL
50 mM 0.0471 mL 0.2356 mL 0.4712 mL 1.1780 mL
60 mM 0.0393 mL 0.1963 mL 0.3927 mL 0.9817 mL
80 mM 0.0294 mL 0.1472 mL 0.2945 mL 0.7362 mL
100 mM 0.0236 mL 0.1178 mL 0.2356 mL 0.5890 mL
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GLPG2534 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:

GLPG25342095615-97-5GLPG 2534GLPG-2534IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseInflammationADTNF-αIL-1βpsoriasisskin diseasesInhibitorinhibitorinhibit

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