2095615-97-5
2095615-97-5 structure
- Name: GLPG2534
- Chemical Name: GLPG2534
- CAS Number: 2095615-97-5
- Molecular Formula: C21H24N6O4
- Molecular Weight: 424.45
- Catalog: Signaling Pathways Immunology/Inflammation IRAK
- Create Date: 2023-05-31 19:36:14
- Modify Date: 2024-01-14 13:02:55
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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].
| Name | GLPG2534 |
|---|
| 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]. |
|---|---|
| Related Catalog | |
| Target |
hIRAK4:6.4 nM (IC50) mIRAK4:3.5 nM (IC50) IRAK1:179 nM (IC50) |
| In Vitro | GLPG2534 抑制 IL-1β 驱动的 IL-6 释放，IC50 为 55 nM[1]。 GLPG2534 抑制 TNF-α 驱动的 IL-6 释放，IC50 为 6.6 μM[1]。 GLPG2534 (0.1-10 μM，16 小时) 抑制鞭毛蛋白刺激的角质形成细胞中 S100A7、DEFB4A、CXCL8、TNF 的表达[1]。 |
| In Vivo | GLPG2534 (0.3-10 mg/kg，口服) 抑制小鼠血液中 CL097 驱动的 TNF-α 释放[1]。 GLPG2534 (10 和 30 mg/kg，口服，每天两次) 减轻银屑病样小鼠模型中的炎症[1]。 GLPG2534 (3-30 mg/kg，p.o.，b.i.d. 5 天) 减轻小鼠 IL-33 和 MC903 诱导的 AD 样皮肤炎症的发展[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%). |
| References |
| Molecular Formula | C21H24N6O4 |
|---|---|
| Molecular Weight | 424.45 |