|2-氨基-7-异丙基-5-氧代-5H-苯并吡喃并[2,3-b]吡啶-3-羧酸|CsnPharm

CAS No.: 68302-57-8

Amlexanox/氨来呫诺 Catalog No. CSN12359

Synonyms: AA673;Amoxanox;CHX3673

Amlexanox is a selective inhibitor of TBK1 and IKKε with IC50 values of ~1-2 μM.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 IKKε

IC50:1-2μM TBK1

IC50:1-2μM
描述E-Amlexanox is a specific inhibitor of IKKε and TBK1(TANK-binding kinase 1), and inhibits the IKKε and TBK1 activity determined by MBP phosphorylation with an IC50 of approximately 1-2 μM. 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^[3]. In primary bone marrow derived macrophages (BMMs), amlexanox inhibited osteoclast formation and bone resorption. At the molecular level, amlexanox suppressed RANKL-induced activation of nuclear factor-κB (NF-κB), mitogen-activated protein kinase (MAPKs), c-Fos and NFATc1. Amlexanox decreased the expression of osteoclast-specific genes, including TRAP, MMP9, Cathepsin K and NFATc1. Moreover, amlexanox enhanced osteoblast differentiation of BMSCs. In ovariectomized (OVX) mouse model, amlexanox prevented OVX-induced bone loss by suppressing osteoclast activity^[4]. Amlexanox significantly inhibited the production of pro-inflammatory mediators, both in vitro and in vivo, while increased interleukin-10 level in LPS-activated macrophages. Mechanistically, amlexanox down-regulated nuclear factor κB and extracellular signal-regulated kinase/activator protein-1 signaling by elevating intracellular 3',5'-cyclic adenosine monophosphate (cAMP) level and subsequently activating protein kinase A^[5].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03237533	Oral Lichen Planus	Early Phase 1	Recruiting	December 31, 2017	Pakistan ... more >> The university of Faisalabad Recruiting Faisalābād, Punjab, Pakistan, 38000 Contact: Sadaf Rashid, BDS +923237791689 durr_e_sadaf@hotmail.com Contact: Arsalan Wahid, M. Phil +923216685228 dr.arsalanmalik@gmail.com Collapse <<
NCT01975935	Diabetes Mellitus Type 2 ... more >> Non-alcoholic Fatty Liver Disease Obesity Collapse <<	Phase 2	Completed	-	United States, Michigan ... more >> University of Michigan Ann Arbor, Michigan, United States, 48109 Collapse <<
NCT01975935	-	-	Completed	-	-

更多
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3524 mL
- 16.7620 mL
- 33.5240 mL
- 5 mM
- 0.6705 mL
- 3.3524 mL
- 6.7048 mL
- 10 mM
- 0.3352 mL
- 1.6762 mL
- 3.3524 mL

技术信息

CAS号

68302-57-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H14N2O4

运输

蓝冰

分子量

298.29

别名

AA673;Amoxanox;CHX3673;Elics;Brand name: Aphthasol;氨来呫诺

溶解度

DMSO	57.0 mg/mL (191.1 mM)
Water	Insoluble
Ethanol	1.0 mg/mL (3.4 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03237533	Oral Lichen Planus	Early Phase 1	Recruiting	December 31, 2017	Pakistan ... more >> The university of Faisalabad Recruiting Faisalābād, Punjab, Pakistan, 38000 Contact: Sadaf Rashid, BDS +923237791689 durr_e_sadaf@hotmail.com Contact: Arsalan Wahid, M. Phil +923216685228 dr.arsalanmalik@gmail.com Collapse <<
NCT01975935	Diabetes Mellitus Type 2 ... more >> Non-alcoholic Fatty Liver Disease Obesity Collapse <<	Phase 2	Completed	-	United States, Michigan ... more >> University of Michigan Ann Arbor, Michigan, United States, 48109 Collapse <<
NCT01975935	-	-	Completed	-	-
NCT01083875	Oral Mucositis	Phase 2	Completed	-	United States, Alabama ... more >> Mobile Infirmary Medical Center Mobile, Alabama, United States, 36607 United States, Arkansas University of Arkansas Medical School Little Rock, Arkansas, United States, 72205 United States, California Florence Wheeler Cancer Center Bakersfield, California, United States, 93301 United States, Connecticut University of Connecticut Health Center Farmington, Connecticut, United States, 06030 United States, Florida ICSL Clinical Studies Melbourne, Florida, United States, 32935 United States, Illinois Loyola University Medical Center Maywood, Illinois, United States, 60115 United States, Massachusetts Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 United States, Michigan Wayne State University School of Medicine Detroit, Michigan, United States, 48201 United States, Tennessee University of Tennessee Memphis, Tennessee, United States, 38163 St. Thomas Hospital Nashville, Tennessee, United States, 37202 United States, Texas Arlington Cancer Center Arlington, Texas, United States, 76012 Corpus Christi Cancer Center Corpus Christi, Texas, United States, 78412 Collapse <<
NCT01842282	Diabetes Mellitus Type 2 ... more >> Non Alcoholic Fatty Liver Disease Obesity Collapse <<	Phase 2	Active, not recruiting	December 2019	United States, Michigan ... more >> University of Michigan Ann Arbor, Michigan, United States, 48109 Collapse <<

靶点	Description	IC50
IKKε		IC50:1-2μM
TBK1		IC50:1-2μM

Amlexanox/氨来呫诺 Catalog No. CSN12359

靶点选择性

请登录您的专属账户

确认信息