IRAK4-IN-21|cas:2170694-04-7|西域试剂

IRAK4-IN-21,99.44%

产品编号：Bellancom-151363| CAS NO：2170694-04-7| 分子式：C₂₈H₂₈FN₇O₂| 分子量：513.57

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-151363		￥4800.00	杭州北京（现货）
Bellancom-151363		￥8000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

IRAK4-IN-21

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 selective IRAK4 inhibitor with IC₅₀ values of 5 and 56 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC₅₀=0.17 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis.

体外研究

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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 IC₅₀ of 0.17 and 0.51 µM, respectively.

Cell Viability Assay

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 IC₅₀ of 0.20 µM.

Cell Viability Assay

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 IC₅₀ of 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.

西域 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).
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.

体内研究

IRAK4-IN-21 (75 mg/kg; p.o.; single) shows moderate efficacy in acute animal model studies for the inhibition of IL-6 production.

西域 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).
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.

体内研究

IRAK4-IN-21 (75 mg/kg; p.o.; single) shows moderate efficacy in acute animal model studies for the inhibition of IL-6 production.

西域 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).
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.