2. Immunology/Inflammation
  3. IRAK
  4. 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.

IRAK4-IN-28 Chemical Structure

IRAK4-IN-28 Chemical Structure

CAS No. : 2952532-92-0

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IRAK4-IN-28 Related Antibodies

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Description

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[1].

IC50 & Target

IC50:8.9 nM (IRAK4)[1], IC50:>30 nM (hERG)[1], Kd:0.58 nM (IRAK4)[1], Kd:140 nM (IRAK1)[1]
In Vitro

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.

IRAK4-IN-28 Related Antibodies

Cell Viability Assay[1]

Cell Line: iBMDM cell
Concentration: 0-33 μM
Incubation Time: 1 h
Result: Reduced mRNA levels and protein levels of TNF-α and IL-6 in mouse iBMDM cells.
In Vivo

IRAK4-IN-28 (compound 42) has favorable pharmacokinetic properties in the SD rat model[1].
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]

大鼠模型中药代动力学分析[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.

Animal Model: LPS-stimulated female C57BL/6 mice[1]
Dosage: 50 or 100 mg/ml, single dose; 1 h prior to 1 mg/kg LPS administration by intraperitoneal injection
Administration: Oral gavage (p.o.)
Result: Inhibited cytokine TNF-α and IL-6 in a dose-dependent manner in an LPS-stimulated mouse model.
Molecular Weight

529.59

Formula

C27H31N9O3
CAS No.
SMILES

CN1N=CC(C2=CC=CC(NC(C3=CC(O4)=C(N=C3N5CCN(C6CC6)CC5)N=C4N7CCOCC7)=O)=N2)=C1
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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IRAK4-IN-28 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:

IRAK4-IN-282952532-92-0IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseInhibitorinhibitorinhibit

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