pgc-1α

ZLN005 is an effective and tissue-specific transcriptional activator of PGC-1α.

ERRα antagonist-1 (ERR+ - antagonist-1) is a high-affinity, selective antagonist of the estrogen-related receptor α (ERRα). It effectively prevents the interaction of ERRα with both Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, displaying IC50 values of 170 nM and 180 nM, respectively. Notably, ERRα antagonist-1 does not interfere with the interactions involving ERRβ or ERRγ and the PGC-1α and PGC-1β coactivators. Furthermore, it does not affect the interaction between either ERα or ERβ and PGC-1α or SRC-1.

Tetrahydroxystilbene-2-O-β-D-glucoside (EH-201) is a low MW inducer of erythropoietin. Tetrahydroxystilbene-2-O-β-D-glucoside induces expression of erythropoietin, PPAR-γ coactivator 1α (PGC-1α) and haemoglobin in astrocytes and PC12 neuronal-like cells. In vivo, Tetrahydroxystilbene-2-O-β-D-glucoside treatment restores memory impairment, as assessed by the passive avoidance test, in SD, Aβ and KA mouse models. In the hippocampus of mice given Tetrahydroxystilbene-2-O-β-D-glucoside in their diet, levels of erythropoietin, PGC-1α and haemoglobin were increased. Treatment with Tetrahydroxystilbene-2-O-β-D-glucoside might be a therapeutic strategy for memory impairment in neurodegenerative disease, physiological ageing or traumatic brain injury.

RGX-202 (β-GPA) is a creatine analog that alters skeletal muscle energy expenditure. It reduces cellular ATP, creatine, and phosphocreatine levels and stimulates AMP-activated protein kinase (AMPK), activating PPARγ coactivator 1α (PGC-1α).

SR-18292 is an inhibitor of PPAR gamma coactivator-1α (PGC-1α), which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.

KL1333 (NQO1 activator 1) enhances energy metabolism and mitochondrial dysfunction in MELAS fibroblasts. Elevated NAD+ levels trigger the activation of SIRT1 and AMPK, and subsequently activates PGC-1α. NQO1 activator 1 is an orally available NAD+ modulator. It reacts with NAD(P)H: NQO1 as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation.

EB1002 is a selective NK2R agonist that has demonstrated significant enhancements in the expression levels of genes associated with mitochondrial biogenesis (such as PGC-1α) in obese mice. This suggests that EB1002 promotes energy expenditure by enhancing mitochondrial activity. Additionally, EB1002 has improved insulin sensitivity and glucose-lipid metabolism in mice. Therefore, EB1002 holds potential for research into obesity and type 2 diabetes.

DS45500853 is a novel ERRα agonist that does not activate PPARγ and promotes the recruitment of PGC-1α coactivating peptide by directly binding to ERRα. It has potential for the treatment of metabolic disorders such as type 2 diabetes.

Ac-SVVVRT-NH2, a PGC-1α modulator, enhances the activity of the human PGC-1α promoter (114%), elevates PGC-1α mRNA levels (125%), and promotes intracellular lipid accumulation (128%) in subcutaneous human adipocytes. This compound has potential applications in research related to diseases influenced by PGC-1α.

Mogroside VI B, a cucurbitane glucoside derived from Siraitia grosvenorii crude extract, exhibits potency in activating PGC-1α transcription [1].

11-Oxoisomogroside V (compound 3), a cucurbitacin derived from Luo Han Guo extract, enhances the transcriptional activity of PGC-1α. Luciferase assay data demonstrates that at concentrations of 10 μM and 20 μM, 11-Oxoisomogroside V increases luciferase activity to 133.79% and 143.81%, respectively [1].

Phoenixin-20 (PNX-20) is a vertebrate bioactive peptide with hormone-like actions, stimulating the hypothalamo-pituitary-gonadal axis to regulate mammalian reproduction, enhancing neuronal mitochondrial biogenesis via the CREB-PGC-1α pathway, and possessing an anxiolytic effect [1] [2] [3].

Phoenixin-20 (TFA) (PNX-20 (TFA)) is a bioactive peptide that stimulates hypothalamo-pituitary-gonadal hormones, regulates mammalian reproductive processes, enhances neuronal mitochondrial biogenesis via the CREB-PGC-1α pathway, and exhibits anxiolytic properties [1] [2] [3].

Gartanin is an androgen receptor degradation enhancer, it is also a potential neuroprotective agent against glutamate-induced oxidative injury partially through increasing Nrf-2-independed HO-1 and AMPK SIRT1 PGC-1α±signaling pathways.