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关于此项目
经验公式(希尔记法):
C20H12N2O3S
化学文摘社编号:
分子量:
360.39
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
产品名称
A-769662, ≥98% (HPLC)
assay
≥98% (HPLC)
form
powder
color
white to very dark brown
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
[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
Biochem/physiol Actions
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Christopher G Langendorf et al.
Nature communications, 7, 10912-10912 (2016-03-10)
The metabolic stress-sensing enzyme AMP-activated protein kinase (AMPK) is responsible for regulating metabolism in response to energy supply and demand. Drugs that activate AMPK may be useful in the treatment of metabolic diseases including type 2 diabetes. We have determined
John W Scott et al.
Chemistry & biology, 15(11), 1220-1230 (2008-11-22)
The AMP-activated protein kinase (AMPK) is an alphabetagamma heterotrimer that plays a pivotal role in regulating cellular and whole-body metabolism. Activation of AMPK reverses many of the metabolic defects associated with obesity and type 2 diabetes, and therefore AMPK is
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