IRAK4-IN-21

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IRAK4-IN-21

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2170694-04-7

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

IRAK4-IN-21 (化合物 17) 是一种口服有效的和具有选择性的强效IRAK4抑制剂，其对IRAK4和TAK1的IC₅₀值分别为 5 和 56 nM。IRAK4-IN-21 能够有效抑制 IL-23 的产生 (IC₅₀=0.17 μM)，可用于自身免疫性疾病，如斑块状银屑病和银屑病关节炎的研究。

生物活性

IRAK4-IN-21 (compound 17) is an orally active, potent and selectiveIRAK4inhibitor withIC₅₀values of 5 and 56 nM forIRAK4andTAK1, respectively. IRAK4-IN-21 effectively inhibitsIL-23production (IC₅₀=0.17 μM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis^[1].

体外研究
(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].

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 IC₅₀of 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 IC₅₀of 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 IC₅₀of 0.47 μM.

体内研究
(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].

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.

分子量

513.57

Formula

C₂₈H₂₈FN₇O₂

CAS 号

2170694-04-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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