AMPK α1β1γ1 Activator

EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with K_ds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.

PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC₅₀ of 7 nM.

PF-739 is an orally active and non-selective activator of AMPK. PF-739 activates 12 heterotrimeric AMPK complexes and significantly reduces the level of glucose in plasma complexes.

PXL770 is an orally active, direct allosteric AMP-activated protein kinase (AMPK) activator. PXL770 decreases C26:0 levels, improves mitochondrial respiration, reduces expression of proinflammatory genes and induces expression of compensatory transporters (ABCD2/3) in ALD fibroblasts/lymphocytes. PXL770 normalizes plasma VLCFA levels, significantly reduces elevated VLCFA levels in brain and spinal cord in Abcd1 KO mice. PXL770 improves glycemia, dyslipidemia, and insulin resistance in ob/ob and high-fat diet (HFD)-fed mice. PXL770 can be used for the study of X-linked adrenoleukodystrophy (ALD), autosomal dominant polycystic kidney disease and nonalcoholic steatohepatitis (NASH).

ZLN024 hydrochloride is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC₅₀s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.

PF-06685249 (PF-249) is a potent and orally active allosteric AMPK activator with an EC₅₀ of 12 nM for recombinant AMPK α1β1γ1. PF-06685249 improves renal function in ZSF-1 rats with diabetic nephropathy. PF-06685249 can be used for diabetic nephropathy research.

AMPKα1 activator 1 is a selective and orally active AMPKα1 activator with an EC₅₀ of 35.1 nM. AMPKα1 activator 1 shows 176-fold selectivity over AMPKα2. AMPKα1 activator 1 can be used as a cell protectant and a kidney protectant. AMPKα1 activator 1 attenuates elevation of serum creatinine and blood urea nitrogen levels, alleviates kidney damage, and reduces cellular infiltration in renal ischemia-reperfusion injury contexts. AMPKα1 activator 1 can be associated with renal ischemia-reperfusion injury research.

AMPK activator 8 (compound 2) is an AMP-activated protein kinase (AMPK) activator with EC₅₀s of 11, 27, 4, 2, and 4 nM for rAMPK α1β1γ1, rAMPK α2β1γ1, rAMPK α1β2γ1, rAMPK α2β2γ1, rAMPK α2β2γ3, respectively. AMPK activator 8 can be used for the research of type 2 diabetes.

BI-9774 is a potent, selective, and orally active AMPK activator, with EC₅₀ values of 20.0 nM and 63.1 nM against human AMPK α1β1γ1 and AMPK α1β2γ1, respectively. BI-9774 binds to the allosteric drug and metabolite (ADaM) site and induces ACC Ser79 phosphorylation in HepG2 cells, with an EC₅₀ of 83.2 nM. BI-9774 can be used in studies related to AMPK signaling, multiple sclerosis, and non-alcoholic fatty liver disease.

PF-06679142 (Compound 10) is a potent, orally active AMPK activator with an EC₅₀ of 22 nM against α1β1γ1-AMPK. PF-06679142 can be used for diabetic nephropathy research.

ZLN024 is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC₅₀s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.