| Identification | Back Directory | [Name]
6-[6-[2-(2-Hydroxyethoxy)ethoxy]-5-[(tetrahydro-2H-pyran-4-yl)amino]-3H-imidazo[4,5-b]pyridin-3-yl]-3-pyridinecarbonitrile | [CAS]
2095615-97-5 | [Synonyms]
6-[6-[2-(2-Hydroxyethoxy)ethoxy]-5-[(tetrahydro-2H-pyran-4-yl)amino]-3H-imidazo[4,5-b]pyridin-3-yl]-3-pyridinecarbonitrile | [Molecular Formula]
C21H24N6O4 | [MOL File]
2095615-97-5.mol | [Molecular Weight]
424.45 |
| Chemical Properties | Back Directory | [Boiling point ]
701.5±70.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted) | [form ]
Solid | [pka]
14.33±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [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].
| 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%). |
| [IC 50]
hIRAK4: 6.4 nM (IC50); mIRAK4: 3.5 nM (IC50); IRAK1: 179 nM (IC50) | [References]
[1] Lavazais S, et al. IRAK4 inhibition dampens pathogenic processes driving inflammatory skin diseases. Sci Transl Med. 2023 Feb 15;15(683):eabj3289. DOI:10.1126/scitranslmed.abj3289 |
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