pgc-1α

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

D-Mannitol (Mannitol) is a diuretic and renal diagnostic aid related to sorbitol. It has little significant energy value as it is largely eliminated from the body before any metabolism can take place. It can be used to treat oliguria associated with kidney failure or other manifestations of inadequate renal function and has been used for determination of glomerular filtration rate. D-Mannitol is also commonly used as a research tool in cell biological studies, usually to control osmolarity.

Metaxalone (Methaxalonum) (marketed by King Pharmaceuticals under the brand name Skelaxin ) is a muscle relaxant used to relax muscles and relieve pain caused by strains, sprains, and other musculoskeletal conditions.

Neuroprotective agent 8 (compound AA-9) is an orally active neuroprotective agent that functions through antioxidant stress reduction and anti-inflammatory mechanisms. In a rat model of MCAO ischemic stroke, it activates PGC-1α and inhibits the NLRP3 inflammasome.

ZLN005 (hydrochloride) is an activator of the peroxisome proliferator-activated receptor-gamma coactivator 1-alpha (PGC-1α). It enhances the expression of PGC-1α and downstream genes in skeletal muscle cells, leading to improved glucose utilization and fatty acid oxidation. In diabetic db/db mice, ZLN005 (hydrochloride) elevates the transcription of PGC-1α and downstream genes in skeletal muscle, boosts fat oxidation, and enhances glucose tolerance, pyruvate tolerance, and insulin sensitivity.

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].

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].

Metaxalone-d6 is intended for use as an internal standard for the quantification of metaxalone by GC-or LC-MS. Metaxalone is a skeletal muscle relaxant. It inhibits the proliferation of, and induces apoptosis in, RAW 264.7 cells in vitro when used at concentrations ranging from 1 to 100 µM. Metaxalone also reduces LPS-induced increases in COX-1, COX-2, and NF-kB levels and inhibits LPS-induced production of TNF-α, IL-6, and prostaglandin E2 in RAW 264.7 cells. Formulations containing metaxalone have been used in the treatment of lower back pain.

AdipoR agonist 1 (Compound 112254), acting as an agonist for the adiponectin receptor (AdipoR), stimulates transcriptional regulators including peroxisome proliferator-activated receptors (PPARs), peroxisome proliferator-activated receptor gamma coactivator 1α (PGC-1α), sirtuin 1 (SIRT1), and adenylate-activated protein kinase (AMPK). It is employed in the field of preventive doping research.

Acetyl hexapeptide 38, breast enhancement peptide, is a kind of acetylated hexapeptide, can significantly stimulate the use of the site of fat synthesis, increase the volume of the chest or cheek, shape the perfect body

Medioresinol possesses antioxidative, a lesishmanicidal activity and cardiovascular disease risk reduction, it has antiamyloidogenic activity via reduction in the amount of α²-secretase, it is a potentially valuable antiamyloidogenic agent for the prevent

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).

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.

KL1333 hydrochloride is an orally effective NAD+ modulator that acts as a substrate for NAD(P)H: quinone oxidoreductase 1 (NQO1), leading to increased intracellular NAD+ levels through NADH oxidation. Elevated NAD+ subsequently activates SIRT1 and AMPK, which in turn activate PGC-1α. KL1333 hydrochloride improves energy metabolism and mitochondrial dysfunction in fibroblasts of mitochondrial encephalomyopathy, lactic acidosis, and stroke-like episodes (MELAS). It also has a protective effect against cisplatin-induced ototoxicity in cultured mouse cochlea.

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.

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].

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.