[CAS NO. 2170694-04-7] IRAK4-IN-21
PRODUCTS SPECIFICATIONS [2170694-04-7]
DESCRIPTION [2170694-04-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 513.57 |
| Molecular Formula | C28H28FN7O2 |
| SMILES | O=C([C@H]1[C@@H](C2)C=C[C@@H]2[C@H]1NC3=NC(NC4=CC=CC(C(N5CCCC5)=O)=C4)=NC=C3C6=CC(F)=CN=C6)N |
Summary
IRAK4-IN-21 (compound 17) is an orally active, potent and selective IRAK4 inhibitor with IC 50 values of 5 and 56 nM for IRAK4 and TAK1 , respectively. IRAK4-IN-21 effectively inhibits IL-23 production ( IC 50 =0.17 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis [1] .
In Vitro
IRAK4-IN-21 (a 4-fold serial dilution from 10 µM; 1 h) decreases the levels of IL-23 (in THP-1 and DC cells), IL-6 (in HUVEC cells) and MIP-1β (in human whole blood) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | THP-1, DC cells (are primed with IFN-γ) |
| Concentration: | 10 µM (a 4-fold serial dilution from 10 µM) |
| Incubation Time: | 1 h (pre-incubate) |
| Result: | Inhibited the levels of IL-23 in the supernatant of THP-1 and DC cells with IC 50 of 0.17 and 0.51 µM, respectively. |
Cell Viability Assay [1]
| Cell Line: | HUVEC cells (IL-1β-stimulated) |
| Concentration: | 10 µM (a 4-fold serial dilution from 10 µM) |
| Incubation Time: | 1 h (pre-incubate) |
| Result: | Inhibited the level of IL-6 in the supernatant of HUVEC cells with an IC 50 of 0.20 µM. |
Cell Viability Assay [1]
| Cell Line: | Human whole blood (IL-1β-stimulated) |
| Concentration: | 10 µM (a 4-fold serial dilution from 10 µM) |
| Incubation Time: | 1 h (pre-incubate) |
| Result: | Inhibited the level of MIP-1β in the human whole blood with an IC 50 of 0.47 µM. |
In Vivo
IRAK4-IN-21 (75 mg/kg; p.o.; single) shows moderate efficacy in acute animal model studies for the inhibition of IL-6 production [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | BALB/c mice (acute mouse model; IL-1β-stimulated) [1] . |
| Dosage: | 75 mg/kg |
| Administration: | Oral administration; single (pre-treat). |
| Result: | Showed 54% inhibition of IL-6, plasma concentrations was 2877 ng/mL at 0.5 h and 496 ng/mL at 2 h. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |