IRAK4-IN-28
IRAK4-IN-28 (compound 42) is an orally active IRAK4 inhibitor (IC50=8.9 nM). IRAK4-IN-28 has binding affinity for IRAK4 with a Kd of 0.58 nM. IRAK4-IN-28 can be used in the research of inflammation and autoimmune diseases.
For research use only. We do not sell to patients.
- CAS No.: 2952532-92-0
- Formula: C27H31N9O3
- Molecular Weight:529.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50:8.9 nM (IRAK4)[1], IC50:>30 nM (hERG)[1], Kd:0.58 nM (IRAK4)[1], Kd:140 nM (IRAK1)[1]
IRAK4-IN-28 (compound 42) has no inhibition on cytochrome P450 enzymes CYP1A2, CYP2D6, CYP3A4, and hERG which means a good safety and ‘drug-likeness’ properties[1].
IRAK4-IN-28 inhibits CYP2C9, CYP2C19 with IC50 of 12 μM and 2.7 μM, respectively[1].
IRAK4-IN-28 has high plasma protein binding in human and rat (99.8 an 97.2, respectively)[1].
IRAK4-IN-28 (1 h) inhibits the LPS (HY-D1056)-induced TNF-α and IL-6 expression at both mRNA and protein levels in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:iBMDM cell
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Concentration:0-33 μM
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Incubation Time:1 h
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Result:Reduced mRNA levels and protein levels of TNF-α and IL-6 in mouse iBMDM cells.
IRAK4-IN-28 has orally bioactive with 68% availability[1].
IRAK4-IN-28 (50 or 100 mg/ml, single dose, oral ) significantly reduces LPS-induced TNF-α and IL-6 cytokines release in the mouse model[1].
Pharmacokinetic Analysis in male SD Rat Model[1]
| Route | Dose (mg/kg) | Clobs (mL·h/kg) | Clmax (ng/mL) | Vss_obs (L/kg) | AUClast (ng·h/mL) | t1/2 (h) | Tmax (h) | F (%) |
| i.v. | 2 | 21 | / | 3.2 | 1520 | 1.8 | / | / |
| p.o. | 10 | / | 1133 | / | 5196 | / | 1.7 | 68 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS-stimulated female C57BL/6 mice[1]
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Dosage:50 or 100 mg/ml, single dose; 1 h prior to 1 mg/kg LPS administration by intraperitoneal injection
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Administration:Oral gavage (p.o.)
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Result:Inhibited cytokine TNF-α and IL-6 in a dose-dependent manner in an LPS-stimulated mouse model.
Chemical Information
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CAS No. 2952532-92-0
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Molecular Weight 529.59
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Formula C27H31N9O3
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SMILES
CN1N=CC(C2=CC=CC(NC(C3=CC(O4)=C(N=C3N5CCN(C6CC6)CC5)N=C4N7CCOCC7)=O)=N2)=C1
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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)
IRAK4-IN-28 Related Classifications
HY-155132 Related Classifications
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