| Cat. No. |
Product Name |
CAS No. |
Information |
| H9245 |
Marein
|
535-96-6 |
Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway; Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects. |
| H9236 |
MT 63-78
|
1179347-65-9 |
MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis; MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects. |
| H6944 |
ZLN-024 hydrochloride
|
1883548-91-1 |
A novel AMPK allosteric activator that has no effect on mitochondrial function or the ADP/ATP ratio; directly activate recombinant AMPK α1β1γ1 and its homologue α2β1γ1 with EC50 of 0.42 uM and 0.95 uM, respectively; also directly activate recombinant AMPK α1β2γ1 (EC50=1.1 µuM) and AMPK α2β2γ1 (EC50=0.13 uM); activates AMPK in L6 myotubes and stimulates glucose uptake and fatty acid oxidation; improves glucose tolerance, liver tissue weight, triacylglycerol and decreases the total cholesterol content in db/db mice (15 mg/kg/day). |
| H6943 |
ZLN-024
|
723249-01-2 |
A novel AMPK allosteric activator that has no effect on mitochondrial function or the ADP/ATP ratio; directly activate recombinant AMPK α1β1γ1 and its homologue α2β1γ1 with EC50 of 0.42 uM and 0.95 uM, respectively; also directly activate recombinant AMPK α1β2γ1 (EC50=1.1 µuM) and AMPK α2β2γ1 (EC50=0.13 uM); activates AMPK in L6 myotubes and stimulates glucose uptake and fatty acid oxidation; improves glucose tolerance, liver tissue weight, triacylglycerol and decreases the total cholesterol content in db/db mice (15 mg/kg/day). |
| H6942 |
PF-739
|
1852452-14-2 |
A novel potent, pan-AMPK activator with similar potency for all AMPK heterotrimers; increases the phosphorylation of the AMPK substrate ACC at S79 with EC50 of 121 nM, potently inhibits de novo lipogenesis (IC50=25 nM) in primary rat hepatocytes; increases PGC1a transcription and mitochondrial content, effectively activats AMPK in hepatocytes and in skeletal muscle; caused a rapid lowering of plasma glucose levels with no impact on hepatic glucose production in diabetic mice. |
| H6941 |
PF-249
|
1467059-70-6 |
PF-249 is a potent, selective AMPK β1-containing complexes activator; increases the phosphorylation of the AMPK substrate ACC at S79 with EC50 of 296 nM, potently inhibits de novo lipogenesis (IC50=15 nM) in primary rat hepatocytes. |
| H6939 |
PF-06685249
|
1467059-70-6 |
PF-06685249 is a novel potent, orally active, α1β1γ1/α2β1γ1-isoform selective AMPK activator with Kd of 14 nM, EC50 of 12 nM for α1β1γ1-AMPK, shows minimal activity at the β2-containing isoforms (α1β2γ1, α2β2γ1, α2β2γ3); demonstrates in vivo target engagement experiment in ZSF-1 rats, an obese/diabetic rodent model of diabetic nephropathy. |
| H6938 |
PF-06679142
|
1467059-66-0 |
PF-06679142 is a novel potent, orally active, α1β1γ1/α2β1γ1-isoform selective AMPK activator with Kd of 14 nM, EC50 of 22 nM for α1β1γ1-AMPK, shows minimal activity at the β2-containing isoforms (α1β2γ1, α2β2γ1, α2β2γ3); demonstrates in vivo target engagement experiment in ZSF-1 rats, an obese/diabetic rodent model of diabetic nephropathy. |
| H6937 |
PF-06409577
|
1467057-23-3 |
PF-06409577(PF06409577, PF 6409577) is a potent, selective AMPK β1-containing isoforms activator with TR-FRET EC50 of 7.0 and 6.8 nM for α1β1γ1 and α2β1γ1, respectively; displays no activity for α1β2γ1/α2β2γ1/α2β2γ3 with EC50 >40 uM; elevates the phosphorylation of AMPK in the kidney, without impacting blood glucose levels, and reduces the progression of proteinuria in rat model of diabetic nephropathy.
|
| H6936 |
MT47-100
|
1179347-23-9 |
A novel potent, allosteric, simultaneously direct activator and inhibitor of AMPK complexes containing the β1 or β2 isoform, respectively; maximally activates α1β1γ1 approximately 2.5-fold with half-maximal activation Ka of 3.7 uM and activates all AMPKβ1 complexes regardless α or γ isoforms; directly inhibits AMPKβ2 complexes independently of α or γ isoforms with Ki of 24.8 uM, this inhibition is dependent on the β2 carbohydrate-binding module (CBM) and independent of β2-Ser108 phosphorylation; augmentes glucose-stimulated insulin secretion from isolated mouse pancreatic islets via a β2-dependent mechanism. |
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