IRAK4-IN-19
IRAK4-IN-19 is a potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC50 value of 4.3 nM. IRAK4-IN-19 can inhibit LPS-induced IL23 production in THP and DC cells, and stop arthritis development in arthritis rats. IRAK4-IN-19 can be used for researching arthritis disease.
For research use only. We do not sell to patients.
- CAS No.: 3032075-32-1
- Formula: C25H26F2N8O
- Molecular Weight:492.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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IRAK4 4.3 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.82 μM
Compound: 39
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Induction of PAD activity against human A549 cells
Induction of PAD activity against human A549 cells
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[PMID: 35863718] |
| Dendritic cell | IC50 |
0.22 μM
Compound: 39
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Antiinflammatory activity against human dendritic cells assessed as inhibition of LPS induced IL-23 production
Antiinflammatory activity against human dendritic cells assessed as inhibition of LPS induced IL-23 production
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[PMID: 35863718] |
| THP-1 | IC50 |
0.23 μM
Compound: 39
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Antiinflammatory activity against human THP-1 cells assessed as inhibition of LPS induced IL-23 production
Antiinflammatory activity against human THP-1 cells assessed as inhibition of LPS induced IL-23 production
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[PMID: 35863718] |
IRAK4-IN-19 (compound 39) has inhibitory activity against LPS-induced IL23 in THP and DC with IC50s of 0.23 and 0.22 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
IRAK4-IN-19 (1 mg/kg for IV, 5 mg/kg for PO, single dosage) exhibits a favorable pharmacokinetics profile[1].
IRAK4-IN-19 (5, 15, 45 and 75 mg/kg) exhibits good efficacy in an acute mouse model for the IL-1β induced IL-6 expression, with 64% inhibition at 75 mg/kg dose, 37% inhibition at 45 mg/kg dose, 16% inhibition at 15 mg/kg dose and 9% inhibition at 5 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:30 mg/kg
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Administration:twice daily for 21 days
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Result:Completely stopped arthritis development in arthritis rats at 30 mg/kg.
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Animal Model:Rats[1]
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Dosage:1 mg/kg, 5 mg/kg
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Administration:IV and PO, single dosage
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Result:Exhibited a favorable pharmacokinetics profile with a clearance of 6 mL/min/kg and oral bioavailability of 43%.
Chemical Information
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CAS No. 3032075-32-1
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Molecular Weight 492.52
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Formula C25H26F2N8O
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SMILES
CC(N1N=CC2=C1C=C(NC(N=C3C=C4)=NC(N[C@H]5[C@@H](C(N)=O)[C@@H]6C=C[C@H]5C6)=C3N4C(F)F)C=C2)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)