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Art. -Nr.: HY-178012

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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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CAS. Nr.: 2499855-36-4
Formel: C₂₂H₂₆N₄O₄
Molecular Weight:410.47

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

GLPG4471 Chemical Structure

CAS. Nr.: 2499855-36-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

IRAK4

1.7 nM (IC₅₀)

Alle IRAK Isoform-spezifische Produkte anzeigen :

Alle TNF Receptor Isoform-spezifische Produkte anzeigen :

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.

Parmacokinetics

Species	Dose	Route	CL	V_ss	T_1/2	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.

Chemical Information

CAS. Nr. 2499855-36-4
Molecular Weight 410.47
Formel C₂₂H₂₆N₄O₄
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mammoliti O, et al. Discovery of GLPG4471, a potent and selective IRAK4 inhibitor for the treatment of inflammatory and autoimmune diseases. Bioorg Med Chem Lett. 2025 Dec 15;129:130386. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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GLPG4471

Alle IRAK Isoform-spezifische Produkte anzeigen

Alle TNF Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

GLPG4471 Related Classifications

HY-178012 Related Classifications