PPARγ Activator

Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research.

Daidzein is a soy isoflavone, which acts as a PPAR activator.

Astaxanthin, the red dietary carotenoid, is an orally effective and potent antioxidant. Astaxanthin inhibits NF-κB and down-regulates VEGF in blood glucose. Astaxanthin exerts anti-cancer cell proliferation, increases apoptosis, impairs migration and invasion by activating PPARγ and reducing the expression of STAT3. Astaxanthin also has neuroprotective and anti-inflammatory activity and can be used in studies of cancer, diabetic retinopathy, cardiovascular disease, and in the coloring of animal feed.

Sodium propionate is an orally active short-chain fatty acid. Sodium propionate can be produced by intestinal bacteria from the metabolism of dietary fiber. Sodium propionate increases PPAR-γ, inhibits NF-κB activation, and reduces COX-2 expression and NO production. Sodium propionate also induces Apoptosis and Autophagy. Sodium propionate reduces HSV-1-induced keratitis. Sodium propionate has anticancer effects against glioblastoma. Sodium propionate exhibits neuroprotective, antioxidant, and anti-inflammatory activities. Sodium propionate can be used in the research of spinal cord injury and Alzheimer's disease.

Glabridin is a natural isoflavan from Glycyrrhiza glabra L., binds to and activates PPARγ, with an EC₅₀ of 6115 nM. Glabridin exhibits antioxidant, anti-bacterial, anti-nephritic, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic, cardiovascular protective, neuroprotective and radical scavenging activities.

Inclisiran sodium is a double-stranded small interfering RNA (siRNA) molecule. Inclisiran sodium inhibits the transcription of PCSK9. Inclisiran sodium inhibits Pyroptosis, activates PPARγ, and reduces NLRP3, cleaved caspase-1, IL-1β, and IL-18. Inclisiran sodium has anti-inflammatory, lipid-regulating and anti-atherosclerotic activities. Inclisiran sodium can be used in researches of hyperlipidemia and cardiovascular disease (CVD).

Inclisiran is a double-stranded small interfering RNA (siRNA) molecule. Inclisiran inhibits the transcription of PCSK9. Inclisiran inhibits Pyroptosis, activates PPARγ, and reduces NLRP3, cleaved caspase-1, IL-1β, and IL-18. Inclisiran has anti-inflammatory, lipid-regulating and anti-atherosclerotic activities. Inclisiran can be used in researches of hyperlipidemia and cardiovascular disease (CVD).

CDDO-Im (RTA-403) is an activator of Nrf2 and PPAR, with K_is of 232 and 344 nM for PPARα and PPARγ.

Alpinetin is a flavonoid isolated from cardamom and possesses antitumor, antiinflammation, hepatoprotective, cardiovascular protective, lung protective, antibacterial, antiviral, neuroprotective properties. Alpinetin inhibits lipopolysaccharide (LPS)-induced inflammation, activates PPAR-γ, activates Nrf2, and inhibits TLR4 expression to protect LPS-induced renal injury.

15-keto-Prostaglandin E2 (15-keto-PGE2) is an endogenous PGE₂ metabolite. 15-keto-Prostaglandin E2 inhibits STAT3 activation by binding to the Cys259 residue of STAT3. 15-keto-Prostaglandin E2 binds to and stabilizes EP2 and EP4 receptors. 15-keto-Prostaglandin E2 inhibits the growth and progression of breast cancer cells. 15-keto-Prostaglandin E2 activates PPAR-γ and promotes fungal growth. 15-keto-Prostaglandin E2 disrupts glomerular vascularization during zebrafish development and reduces the surface area of the glomerular filtration barrier.

D-Arabinose is is an orally active antidepressant and a growth inhibitor of C. elegans (IC₅₀ is 7.5 mM). D-Arabinose can penetrate the blood-brain barrier, selectively interfere with the metabolism of D-ribose and D-fructose, and inhibit the growth of nematodes. D-Arabinose can also inhibit the synthesis of cell biofilm and exert antibacterial activity. D-Arabinose activates the ACSS2-PPARγ/TFEB-CRTC1 axis through the lysosomal AXIN-LKB1-AMPK pathway, inducing CRTC1 transcription, exerts antidepressant-like activity. D-Arabinose is the ring-opened form of the aldopentose D-Arabinose (HY-N7082).

Perfluorobutanesulfonic acid (PFBS) is a short-chain perfluoroalkyl substance and the main replacement for perfluorooctanesulfonic acid. Perfluorobutanesulfonic acid induces fat accumulation in human HepG2 hepatoma cells. Perfluorobutanesulfonic acid promotes lipid accumulation by activating PPARγ pathway and triggering oxidative stress, endoplasmic reticulum stress and calcium dyshomeostasis. Perfluorobutanesulfonic acid impairs reproduction and causes developmental disorders in offspring of Caenorhabditis elegans. Perfluorobutanesulfonic acid disrupts pancreatic organogenesis and lipid homeostasis in zebrafish embryos. Perfluorobutanesulfonic acid can be used in environmental toxicology, lipid metabolism and developmental toxicity studies.

γ‑Glutamylvaline (γ-Glu-Val) is a calcium‑sensing receptor (CaSR) agonist. γ‑Glutamylvaline activates CaSR and facilitates its binding to β‑arrestin 2 to modulate inflammatory and metabolic homeostasis signaling. γ‑Glutamylvaline inhibits TNF‑α‑induced IL‑6/MCP‑1 and enhances adiponectin/PPARγ in adipocytes. γ‑Glutamylvaline upregulates Wnt5a, restores β‑catenin phosphorylation, and reduces serine‑phosphorylated IRS‑1 in adipocytes. γ-Glutamylvaline can be used for the research of low-grade chronic inflammation.

Daidzein (Standard) is the analytical standard of Daidzein. This product is intended for research and analytical applications. Daidzein is a soy isoflavone, which acts as a PPAR activator.

SDPC (DHA-PC) is a new generation of omega-3 lipids, which contains an ester bond linking DHA at the sn-2 position of phospholipid. 1-Stearoyl-2-docosahexaenoyl-sn-glyerco-3-phosphocholine exerts anti-angiogenesis effect through activating PPARγ. 1-Stearoyl-2-docosahexaenoyl-sn-glyerco-3-phosphocholine significantly declines the proliferation, migration, tube formation of human umbilical vein endothelial cells. 1-Stearoyl-2-docosahexaenoyl-sn-glyerco-3-phosphocholine has the potential for anti-tumor angiogenesis research.

Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity. Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence.

Oroxylin A-7-O-glucuronide (oroxyloside) is an orally active flavonoid glucuronide and metabolite of Oroxylin A (HY-N0560). Oroxylin A-7-O-glucuronide can be extracted from the dried root of Scutellaria baicalensis. Oroxylin A-7-O-glucuronide exhibits prolyl oligopeptidase inhibitory activity. Oroxylin A-7-O-glucuronide inhibits the JNK pathway, upregulates PPARγ, and inhibits NF-κB p65 nuclear translocation. Oroxylin A-7-O-glucuronide reduces cytokine (IL-1β, IL-6) production. Oroxylin A-7-O-glucuronide exhibits anti-angiogenic, anti-tumor (glioma, liver cancer), anti-inflammatory, and hepatoprotective activities.

Licarin B, a nitric oxide production inhibitor extracted from the component of the seeds of Myristica fragrans, improves insulin sensitivity via PPARγ and activation of GLUT4 in the IRS-1/PI3K/AKT pathway.

17-HDHA is a DHA-derived specialized pro-resolving mediator (SPM). 17-HDHA inhibits NF-κB activation by activating PPARγ and upregulating IκBα, targets FPR2 and Bcl-6, and also acts as a precursor of RvD1 and PD1. 17-HDHA inhibits pulmonary artery smooth muscle cell proliferation, regulates the expression of adiponectin, GLUT-4 and inflammatory cytokines, suppresses IgE production by B cells and promotes antibody secretion. 17-HDHA reduces adipose tissue inflammation, improves insulin sensitivity and glucose tolerance, alleviates pathological processes associated with pulmonary hypertension, and enhances antibody responses and virus neutralizing activity against influenza HA. 17-HDHA can be used in research related to obesity-associated inflammation, insulin resistance, glucose intolerance, pulmonary hypertension and influenza virus infection.

Falcarindiol, an orally active polyacetylenic oxylipin, activates PPARγ and increases the expression of the cholesterol transporter ABCA1 in cells. Falcarindiol induces apoptosis and autophagy. Falcarindiol has anti-inflammatory, antifungal, anticancer and antidiabetic properties. Falcarindiol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.