GLPG2534
Based on 1 Customer Validation
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.
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- Purity: 98.73%
- CAS No.: 2095615-97-5
- 화학식: C21H24N6O4
- 분자량:424.45
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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Kinase Inhibitor Library
HY-L009
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Pyroptosis Compound Library
HY-L059
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Highly Selective Inhibitors Library
HY-L158
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Serine/Threonine Kinase Inhibitor Library
HY-L164
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Protein Kinase Compound Library
HY-L196
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High-Throughput Bioactive Compound Library
HY-L205
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Anti-Rheumatic Arthritis Compound Library
HY-L210
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Posttranslational Modification Library
HY-L226
Biological Activity
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hIRAK4 6.4 nM (IC50) |
mIRAK4 3.5 nM (IC50) |
IRAK1 179 nM (IC50) |
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 (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.
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Animal Model:Psoriasis-like skin inflammation model, induced by IL-23 and IMQ[1]
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Dosage:10 and 30 mg/kg
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Administration:p.o., b.i.d. 5 days
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Result:Reduced IL-23-induced expression of pathogenic cytokines such as Il17a (79%), Il22 (49%), Il1b (97%), and defensin Lcn2 (69%).
Chemical Information
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CAS No. 2095615-97-5
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Appearance Solid
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분자량 424.45
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화학식 C21H24N6O4
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Color Light yellow to yellow
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SMILES
N#CC(C=N1)=CC=C1N2C3=NC(NC4CCOCC4)=C(OCCOCCO)C=C3N=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 33.33 mg/mL (78.53 mM; ultrasonic and warming and heat to 60°C; 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 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.
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.
순도&문서
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Data Sheet (278 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 |
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| 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 |
GLPG2534 Related Classifications
HY-153224 Related Classifications
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