AMPK
In eukaryotic cells AMP-activated protein kinase (AMPK) plays a major role in regulating cellular energy balance. AMPK responds to changes in intracellular adenine nucleotide levels, being activated by an increase in AMP/ADP relative to ATP.Mammalian AMPK exists as 12 different complexes composed of different subunit isoforms. AMPK is activated by phosphorylation of threonine 172 (T172) within the activation segment of the KD of the a subunit. In mammals, calcium/calmodulin dependent protein kinase kinase (CaMKK) b and liver kinase B1 (LKB1) have been identified as the two upstream kinases in the cascade.AMPK plays an important role in maintaining energy homeostasis in eukaryotic cells. In multicellular organisms, the role of AMPK has been adapted to play a role in integrating energy metabolism at an organismal level.There has been a significant development over the last few years in identifying small molecule direct AMPK activators, and we now understand the mechanism by which a major class of these drugs work to activate the kinase.
References
1.Carling D. Curr Opin Cell Biol. 2017 Apr;45:31-37.
References
1.Carling D. Curr Opin Cell Biol. 2017 Apr;45:31-37.
Membrane Transporter/Ion Channel
AMPK(58)
ASBT Transporter(6)
BCRP(10)
Beta Amyloid(69)
Carbonic Anhydrase(40)
Chloride Channel(34)
CRAC Channel(0)
CRM1(5)
Exportin-1(5)
FABP(6)
GAT(63)
GLUT(5)
Glutamate Transporter(1)
GlyT(13)
HCN Channel(5)
iGluR(52)
Monoamine Transporter(26)
Monocarboxylate Transporter(12)
MTP(1)
nAChR(5)
NADPH(35)
Na-K-ATPase(2)
NKCC(4)
NMDAR(65)
OCT(4)
Other Targets(13)
P2X Receptor(23)
P-glycoprotein(14)
Potassium Channel(0)
Proton Pump(38)
Sodium Channel(147)
TRP/TRPV Channel(115)
URAT1(1)
AMPK
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AMPK activator 12
产品货号 : M37213
cas no: 431920-24-0
AMPK activator 12 (化合物 21) 是一种有效的 AMPK 激活剂和 GDF15 诱导剂。AMPK activator 12 可增加人肝细胞中的 GDF15 蛋白水平。 -
AMPK activator 4
产品货号 : M35625
cas no: 2493239-46-4
AMPK activator 4 是一种有效 AMPK 激活剂,并且不抑制线粒体复合物 I。AMPK activator 4 选择性地激活肌肉组织中的 AMPK。AMPK activator 4 剂量依赖性地改善正常小鼠的糖耐量,显著降低 db/db 糖尿病小鼠的空腹血糖水平和改善胰岛素抵抗。具有降血糖作用。 -
N,N-Didesethyl Sunitinib Hydrochloride
产品货号 : M35336
cas no: 873077-70-4
N,N-Didesethyl Sunitinib Hydrochloride is a potent AMPK inhibitor with IC50 of 393 nM and 141 nM for AMPKα1 and AMPK2,respectively. -
Aldometanib
产品货号 : M35330
cas no: 2904601-67-6
Aldometanib (LXY-05-029) 是一种醛缩酶抑制剂。Aldometanib 可以激活溶酶体腺苷-磷酸活化蛋白激酶 AMPK 并降低血糖。Aldometanib 可用于代谢稳态的研究。 -
YLF-466D
产品货号 : M33176
cas no: 1273323-67-3
YLF-466D 是一种新型 AMPK 激活剂,可抑制血小板聚集。