SML2578
A-769662
≥98% (HPLC)
别名:
4-Hydroxy-3-(2′-hydroxy-1,1′-biphenyl-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile, 4-Hydroxy-3-(2′-hydroxybiphenyl-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile, 6,7-Dihydro-4-hydroxy-3-(2′-hydroxy[1,1′-biphenyl]-4-yl)-6-oxothieno[2,3-b]pyridine-5-carbonitrile, A 769662, A769662
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About This Item
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方案
≥98% (HPLC)
表单
powder
颜色
white to very dark brown
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
[s]1c2[nH][c](c(c(c2c(c1)c3ccc(cc3)c4c(cccc4)O)O)C#N)=O
InChI
1S/C20H12N2O3S/c21-9-14-18(24)17-15(10-26-20(17)22-19(14)25)12-7-5-11(6-8-12)13-3-1-2-4-16(13)23/h1-8,10,23H,(H2,22,24,25)
InChI key
CTESJDQKVOEUOY-UHFFFAOYSA-N
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生化/生理作用
A-769662 is a potent, β1 subunit-selective, allosteric drug and metabolite (ADaM) site AMPK activator (α1β1γ1 EC50/Emax = 0.15 μM/1.99 vs. 4.51 μM/2.19 with AMP) that promotes a Thr172 phosphorylation in a β1 carbohydrate binding module (CBM) Ser108 phosphorylation-dependent manner. A769662 synergizes with AMP as well as C2 (AMP mimetic) toward Thr172 dephosphorylated/Ser108 phosphorylated AMPK. A-769662 is widely employed in probing AMPK β1 complexes-mediated cellular signaling in cultures (conc range: 1 μM-1 mM) as well as AMPK-dependent physiological and pathological processes in mice and rats in vivo (dosing range: 1-30 mg/kg i.p.).
Potent, β1-selective, allosteric drug and metabolite (ADaM) site AMP-activated protein kinase (AMPK) activator in cultures and in vivo.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Davide Di Fusco et al.
Clinical science (London, England : 1979), 132(11), 1155-1168 (2018-03-16)
Metformin, a hypoglycemic drug used for treatment of type 2 diabetes, regulates inflammatory pathways. By using several models of intestinal inflammation, we examined whether metformin exerts anti-inflammatory effects and investigated the basic mechanism by which metformin blocks pathologic signals. Colitic
Nadia Boudaba et al.
EBioMedicine, 28, 194-209 (2018-01-19)
Nonalcoholic fatty liver disease is a highly prevalent component of disorders associated with disrupted energy homeostasis. Although dysregulation of the energy sensor AMP-activated protein kinase (AMPK) is viewed as a pathogenic factor in the development of fatty liver its role
Frank A Duca et al.
Nature medicine, 21(5), 506-511 (2015-04-08)
Metformin is a first-line therapeutic option for the treatment of type 2 diabetes, even though its underlying mechanisms of action are relatively unclear. Metformin lowers blood glucose levels by inhibiting hepatic glucose production (HGP), an effect originally postulated to be
Matthew J Sanders et al.
The Journal of biological chemistry, 282(45), 32539-32548 (2007-08-31)
AMP-activated protein kinase (AMPK) plays a key role in maintaining energy homeostasis. Activation of AMPK in peripheral tissues has been shown to alleviate the symptoms of metabolic diseases, such as type 2 diabetes, and consequently AMPK is a target for
Kerui Fan et al.
Frontiers in immunology, 9, 1464-1464 (2018-07-11)
AMP-activated protein kinase (AMPK) is a crucial metabolic regulator with profound modulatory activities on inflammation. Although the anti-inflammatory benefits of AMPK activators were well documented in experimental studies, the pathological significance of endogenous AMPK in inflammatory disorders largely remains unknown.
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