您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Amlexanox(AA673)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Amlexanox(AA673)
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。
Amlexanox(AA673)图片
CAS NO:68302-57-8
规格:98%
分子量:298.29
包装与价格:
包装价格(元)
10mg电议
50mg电议
100mg电议

产品介绍
AmLexanox是特异性的IKKε和TBK1抑制剂,IC50值为1-2μM。
CAS:68302-57-8
分子式:C16H14N2O4
分子量:298.29
纯度:98%
存储:Store at -20°C

Background:

AmLexanox is a specific inhibitor of IKKε and TBK1, and inhibits the IKKε and TBK1 activity determined by MBP phosphorylation with an IC50 of approximately 1-2 μM.


AmLexanox increases phosphorylation of TBK1 on Ser172 in 3T3-L1 adipocytes, and blocks polyinosinic:polycytidylic acid (poly I:C)-stimulated phosphorylation of interferon responsive factor-3 (IRF3), a presumed substrate of IKKε and TBK1[1]. AmLexanox potently inhibits the release of histamine and leukotrienes from mast cells, basophils and neutrophils in in vitro settings, possibly through increasing intracellular cyclic AMP content in inflammatory cells, a mem-brane-stabilising effect or inhibition of calcium influx[2]. In primary bone marrow derived macrophages (BMMs), amLexanox inhibits osteoclast formation and bone resorption. At the molecular level, amLexanox suppresses RANKL-induced activation of nuclear factor-κB (NF-κB), mitogen-activated protein kinase (MAPKs), c-Fos and NFATc1. AmLexanox decreases the expression of osteoclast-specific genes, including TRAP, MMP9, Cathepsin K and NFATc1[3].


AmLexanox (100 mg/kg, p.o.) prevents and reverses diet-induced or genetic obesity, and produces reversible weight loss in obese mice. AmLexanox also causes a significant decrease in adipose tissue mass in these mice, and an increase in circulating adiponectin. AmLexanox (25 mg/kg) significantly improves insulin sensitivity in mice with established DIO,and after four weeks of treatment, amLexanox produces marked improvements in glucose[1]. AmLexanox before the first application of the paste and at each has been shown to suppress both immediate and evaluation thereafter. A categorical scale is also delayed-type hypersensitivity reactions[2]. AmLexanox (20 mg/kg) enhances osteoblast differentiation of BMSCs. In ovariectomized (OVX) mouse model, amLexanox prevents OVX-induced bone loss by suppressing osteoclast activity[3].


[1]. Reilly SM, et al. An inhibitor of the protein kinases TBK1 and IKK-e improves obesity-related metabolic dysfunctions in mice. Nat Med. 2013 Mar;19(3):313-21. [2]. Bell, J. AmLexanox for the treatment of recurrent aphthous ulcers. Clin Drug Investig, 2005. 25(9): p. 555-66. [3]. Zhang Y, et al. AmLexanox Suppresses Osteoclastogenesis and Prevents Ovariectomy-Induced Bone Loss. Sci Rep. 2015 Sep 4;5:13575.