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AS-2444697(hydrochloride)
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。
AS-2444697(hydrochloride)图片
规格:98%
分子量:432.9
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
An IRAK4 inhibitor
货号:ajcx20388
CAS:1287665-60-4
分子式:C19H20N6O4.HCl
分子量:432.9
溶解度:Soluble in DMSO
纯度:98%
存储:Store at -20°C
库存:现货

Background:

AS-2444697 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4; IC50 = 21 nM).1 It is greater than 30-fold selective for IRAK4 over a panel of 146 kinases, but is less than 10-fold selective over PDGFRα, PDGFRβ, TrkA, TrkC, CLK1, Itk, and FLT3. AS-2444697 inhibits IL-1β-induced IL-6 production and LPS-induced TNF-α production in cellular assays (IC50s = 250 and 47 nM, respectively). It is efficacious in rat models of adjuvant- and collagen-induced arthritis (ED50s = 2.7 and 1.6 mg/kg, respectively). AS-2444697 (0.3-3 mg/kg, twice daily) reduces urinary protein excretion, the development of interstitial fibrosis and glomerulosclerosis, and renal mRNA expression of genes encoding IL-1β, IL-6, TNF-α, and chemokine (C-C motif) ligand 2 (CCL2) without affecting blood pressure in the 5/6 nephrectomized rat model of chronic kidney disease.2


|2. Kondo, M., Tahara, A., Hayashi, K., et al. Renoprotective effects of novel interleukin-1 receptor-associated kinase 4 inhibitor AS2444697 through anti-inflammatory action in 5/6 nephrectomized rats. Naunyn Schmiedebergs Arch. Pharmacol. 287(10), 909-919 (2014).