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GLPG2534 is an orally active, selective and potent IRAK4 inhibitor with anti-inflammatory activity. GLPG2534 inhibits human and mouse IRAK4 and could be used to study psoriasis and atopic dermatitis.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $113 | In Stock | |
5 mg | $278 | In Stock | |
10 mg | $455 | In Stock | |
25 mg | $886 | In Stock | |
50 mg | $1,450 | In Stock | |
100 mg | $2,320 | In Stock |
Description | GLPG2534 is an orally active, selective and potent IRAK4 inhibitor with anti-inflammatory activity. GLPG2534 inhibits human and mouse IRAK4 and could be used to study psoriasis and atopic dermatitis. |
Targets&IC50 | IL-1β:55 nM, IRAK1:179 nM, mIRAK4:3.5 nM, hIRAK4:6.4 nM |
In vitro | GLPG2534 inhibits IL-6 release driven by IL-1β with an IC50 of 55 nM[1]. It also inhibits TNF-α-driven IL-6 release, with an IC50 of 6.6 μM[1]. When applied at concentrations ranging from 0.1 to 10 μM for 16 hours, GLPG2534 inhibits the expression of S100A7, DEFB4A, CXCL8, and TNF in ciliated epithelial cells stimulated with ciliogenesis-promoting factors[1]. |
In vivo | GLPG2534, administered orally at doses ranging from 0.3 to 10 mg/kg, inhibits CL097-driven TNF-α release in mouse blood[1]. Furthermore, oral administration of GLPG2534 at doses of 10 and 30 mg/kg, twice daily, alleviates inflammation in a psoriasis-like mouse model[1]. Additionally, GLPG2534, at doses of 3-30 mg/kg, orally administered twice daily for 5 days, mitigates the development of IL-33 and MC903-induced atopic dermatitis-like skin inflammation in mice[1]. |
Alias | GLPG-2534 |
Molecular Weight | 424.45 |
Formula | C21H24N6O4 |
Cas No. | 2095615-97-5 |
Smiles | N#CC1=CN=C(C=C1)N2C=NC=3C=C(OCCOCCO)C(=NC32)NC4CCOCC4 |
Storage | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (188.48 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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