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Amlexanox

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Chemical Structure| 68302-57-8 同义名 : 氨来诺 ;AA673;Amoxanox;Amoxanox, Brand name: Aphthasol.;Elics;CHX3673
CAS号 : 68302-57-8
货号 : A228799
分子式 : C16H14N2O4
纯度 : 98%
分子量 : 298.293
MDL号 : MFCD00864790
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(352 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
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 ... 展开 >> 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 收起 <<
NCT01975935 Diabetes Mellitus Type 2 ... 展开 >> Non-alcoholic Fatty Liver Disease Obesity 收起 << Phase 2 Completed - United States, Michigan ... 展开 >> University of Michigan Ann Arbor, Michigan, United States, 48109 收起 <<
NCT01975935 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.35mL

0.67mL

0.34mL

16.76mL

3.35mL

1.68mL

33.52mL

6.70mL

3.35mL
参考文献

[1]Zhang Y, Guan H, et al. Amlexanox Suppresses Osteoclastogenesis and Prevents Ovariectomy-Induced Bone Loss. Sci Rep. 2015 Sep 4;5:13575.

[2]Reilly SM, Chiang SH, et al. An inhibitor of the protein kinases TBK1 and IKK-ɛ improves obesity-related metabolic dysfunctions in mice. Nat Med. 2013 Mar;19(3):313-21.

[3]Reilly SM, Chiang SH, Decker SJ, Chang L, Uhm M, Larsen MJ, Rubin JR, Mowers J, White NM, Hochberg I, Downes M, Yu RT, Liddle C, Evans RM, Oh D, Li P, Olefsky JM, Saltiel AR. An inhibitor of the protein kinases TBK1 and IKK-ɛ improves obesity-related metabolic dysfunctions in mice. Nat Med. 2013 Mar;19(3):313-21

[4]Zhang Y, Guan H, Li J, Fang Z, Chen W, Li F. Amlexanox Suppresses Osteoclastogenesis and Prevents Ovariectomy-Induced Bone Loss. Sci Rep. 2015 Sep 4;5:13575

[5]Han Y, Hou R, Zhang X, Liu H, Gao Y, Li X, Qi R, Cai R, Qi Y. Amlexanox exerts anti-inflammatory actions by targeting phosphodiesterase 4B in lipopolysaccharide-activated macrophages. Biochim Biophys Acta Mol Cell Res. 2020 Oct;1867(10):118766