2. Immunology/Inflammation Apoptosis
  3. IRAK TNF Receptor
  4. GLPG4471

GLPG4471 is a selective and orally active IRAK4 inhibitor with an IC50 of 1.7 nM. GLPG4471 exhibits potent inhibition of cytokine (TNFα and IFNα) secretion in cellular and whole blood phenotypic assays. GLPG4471 displays significant activity in a mouse model of collagen-induced arthritis. GLPG4471 can be used for the study of arthritis.

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GLPG4471

GLPG4471 Chemical Structure

CAS No. : 2499855-36-4

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GLPG4471 Related Antibodies

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IRAK1 IRAK3 IRAK4

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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Description

GLPG4471 is a selective and orally active IRAK4 inhibitor with an IC50 of 1.7 nM. GLPG4471 exhibits potent inhibition of cytokine (TNFα and IFNα) secretion in cellular and whole blood phenotypic assays. GLPG4471 displays significant activity in a mouse model of collagen-induced arthritis. GLPG4471 can be used for the study of arthritis[1].

IC50 & Target[1]

IRAK4

1.7 nM (IC50)

In Vitro

GLPG4471 potently inhibits secretion of TNFα and IFNα in human whole blood and PBMCs stimulated with CL097 (HY-128799)[1].
GLPG4471 exhibits excellent metabolic stability in the liver microsomes and liver cells of mice, rats and humans, and the predicted hepatic clearance rate was low to moderate[1].

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

GLPG4471 Related Antibodies
Parmacokinetics
Species Dose Route CL Vss T1/2 F
Mice[1] 1 mg/kg i.v. 0.89 L/h/kg 1.7 L/kg 1.4 h /
Mice[1] 10 mg/kg p.o. / / / 75 %
Rat[1] 0.5 mg/kg i.v. 0.365 L/h/kg 1.7 L/kg 3.1 h /
Rat[1] 5 mg/kg p.o. / / / 87 %
In Vivo

GLPG4471 (3-30 mg/kg, p.o., twice daily for 17 days) displays dose-dependent activity in a mouse model of Collagen (HY-NP010)-induced arthritis[1].

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

Animal Model: Collagen-induced arthritis (CIA) model established in mice[1]
Dosage: 3, 10, 30 mg/kg
Administration: Oral administration (p.o.), twice daily for 17 days
Result: Exhibited a dose-dependent manner of significantly inhibiting the progression of arthritis.
Was above mouse whole blood IC50 for 15, 19 and 24 h at 3, 10 and 30 mg/kg twice-daily, respectively.
Molecular Weight

410.47

Formula

C22H26N4O4
CAS No.
SMILES

COC1=CN2N=C(C=C2C=C1NC(C3=CC=CN(C3=O)C4CC4)=O)CCC(C)(O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GLPG4471 Related Classifications

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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:

GLPG44712499855-36-4GLPG 4471GLPG-4471IRAKTNF ReceptorInterleukin-1 receptor associated kinaseIL-1R associated kinaseTumor Necrosis Factor ReceptorTNFRIRAK4Kinase inhibitorInflammationCollagen-induced arthritisInhibitorinhibitorinhibit

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