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Referencia número: 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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No. CAS: 2499855-36-4
Fòrmula: C₂₂H₂₆N₄O₄
Peso molecular:410.47

Almacenamiento:

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

Data Sheet (274 KB)

GLPG4471 Chemical Structure

No. CAS: 2499855-36-4

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
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Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

IRAK4

1.7 nM (IC₅₀)

Ver todos los productos específicos de isoformas IRAK :

Ver todos los productos específicos de isoformas TNF Receptor :

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

No. CAS 2499855-36-4
Peso molecular 410.47
Fòrmula C₂₂H₂₆N₄O₄
SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (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)
Instrucciones de manejo (2659 KB)

Referencias

[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]

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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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Actividad biológica
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- In Vitro
- In Vivo
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GLPG4471

Ver todos los productos específicos de isoformas IRAK

Ver todos los productos específicos de isoformas TNF Receptor

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

GLPG4471 Related Classifications

HY-178012 Related Classifications