adipocytes

Suksdorfin has hypoglycemic effects, promotes adipocyte differentiation and enhances lipocalin production, activates peroxisome proliferator-activated receptor gamma (PPARγ), promotes insulin-dependent glucose uptake by adipocytes, and can be used to study obesity.

Ketoprofen (RP-19583) is a propionic acid derivative and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. It inhibits cyclo-oxygenase I and II, decreasing the formation of prostaglandin and thromboxane precursors. This reduction in prostaglandin synthesis, mediated by prostaglandin synthase, is responsible for its therapeutic effects. Additionally, Ketoprofen decreases thromboxane A2 formation via thromboxane synthase, inhibiting platelet aggregation.

1. Stearic acid (Cetylacetic acid) can reduce metastatic tumor burden. 2. Stearic acid leads to dramatically reduced visceral fat likely by causing the apoptosis of preadipocytes. 3. Stearic acid and its derivatives have been used as gelators in food and pharmaceutical gel formulations. 4. Stearic acid is a potent phosphatase 1B inhibitor, possibly causing an enhancement in the insulin receptor signaling to stimulate glucose uptake into adipocytes. 5. Stearic acid has the potential to increase dry matter intake and yields of milk and milk components, without affecting conversion of feed to milk, body condition score, or body weight.

Glibenclamide (Glyburide) is an antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.

Rhododendrol (Frambinol) is a melanin synthesis and acts by preventing high-fat diet-induced elevation in body weight and increasing lipolysis in white adipocytes in male mice. Rhododendrol can be used as the lightening whitening cosmetics inhibitor.

Spexin acetate is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Exhibits no significant activity at galanin receptor 1. Endogenous satiety-inducing peptide; inhibits long chain fatty acid uptake by ad

LI-2242 is a potent inositol hexakisphosphate kinase (IP6K) inhibitor with IC50s of 31 nM, 42 nM, 8.7 nM, and 1944 nM for IP6K1, IP6K2, IP6K3, and IPMK, respectively.LI-2242 ameliorated hepatic steatosis by reducing the expression of genes that enhance lipid uptake, lipid stabilization, and adipogenesis, and enhanced mitochondrial oxygen consumption rate (OCR) and insulin signaling in adipocytes and hepatocytes in vitro. LI-2242 ameliorated diet-induced obesity, hyperglycemia and hepatic steatosis in mice.LI-2242 can be used to study type II diabetes, obesity, metabolic complications, venous thrombosis and psychiatric disorders.

13-Methylberberine chloride shows anti-adipogenic effect on 3T3-L1 adipocytes, it has potential as an anti-obesity drug

WWL229 is a selective inhibitor of Ces3, acting by inhibiting recombinant Ces3 while not affecting Ces1f, ABHD6, or other tested serine hydrolases, and replicating the effects of WWL113 in adipocytes.

Naringenin chalcone (Isosalipurpol) has antiallergic activity Naringenin chalcone suppresses asthmatic symptoms by inhibiting Th2 cytokine production from CD4 T cells. Naringenin chalcone is a potent tomato flavonoid that improves adipocyte metabolic functions and exerts insulin-sensitizing effects by activating an adiponectin-related pathway. Naringenin chalcone exhibits anti-inflammatory properties by inhibiting the production of proinflammatory cytokines in the interaction between adipocytes and macrophages, may be useful for ameliorating the inflammatory changes in obese adipose tissue.

TUG-891 is a G protein-coupled receptor (GPCR) expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids.

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.

Pyruvate carboxylase, a biotin-containing enzyme, catalyzes the carboxylation of pyruvate to oxaloacetate, a reaction dependent on HCO3− and MgATP. This enzyme is crucial for regulating whole-body energetics, influencing gluconeogenesis in the liver, fatty acid synthesis in adipocytes, and insulin secretion in pancreatic β-cells [1] [2].

AZD6482 (S-isomer) is a potent, selective, ATP-competitive PI3Kβ inhibitor (IC(50) 0.01 μm), which can inhibit insulin-induced in vitro glucose uptake by human adipocytes (IC(50) is 4.4 μm).

(±)12(13)-DiHOME is the diol form of (±)12(13)-EpOME , a cytochrome P450-derived epoxide of linoleic acid also known as isoleukotoxin. [1] It is formed from 12(13)-EpOME by soluble epoxide hydrolase (sEH) in neutrophils. [2] 12(13)-DiHOME is toxic to Sf21 cells expressing sEH and to lacZ-expressing control cells, unlike isoleukotoxin, which is only toxic to cells containing sEH.[1] [2] Levels of 12(13)-DiHOME are increased in rat spinal cord following burn injury, and it enhances cold tolerance, increases fatty acid uptake into brown adipocytes, and decreases serum triglyceride levels in mice. Levels are also elevated in bronchoalveolar lavage fluid (BALF) in humans following exposure to biodiesel exhaust and in exhaled breath condensate in patients with allergic asthma following allergen exposure.[5] [6] Plasma levels of 12(13)-DiHOME are increased immediately following moderate-intensity exercise in mice and humans, an effect that can be prevented by brown adipose tissue removal in the mouse.[7]

3-Aminoisobutyric acid, a non-protein amino acid resultant from thymine catabolism, plays a significant role in metabolic activities. At a 5 µM concentration, it triggers browning in primary adipocytes, notably elevating uncoupling protein 1 (UCP-1) and CIDEA expression. Additionally, it boosts PPARα expression in both primary adipocytes and mouse inguinal white adipose tissue (WAT) in vivo, alongside enhancing β-oxidation in hepatocytes. Its plasma levels surge post-exercise in mice, and its administration at 100 mg/kg daily curtails weight gain and body fat without diminishing food consumption or hiking energy output, whilst ameliorating glucose tolerance. Notably, 3-aminoisobutyric acid concentrations are heightened in individuals with β-ureidopropionase deficiency, a genetic flaw impairing pyrimidine degradation, affecting plasma, urine, and cerebrospinal fluid.

L 858051 activates adenylate cyclase. It also inhibits glucose transport in rat adipocytes.

Ganglioside GM3 is a monosialoganglioside that demonstrates antiproliferative and proapoptotic effects in tumor cells by modulating cell adhesion, proliferation, and differentiation. It suppresses angiogenesis and reduces proliferation and migration of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 20 μM via inhibition of VEGFR2 and Akt phosphorylation. Ganglioside GM3 induces dissociation of the insulin receptor-caveolin-1 complex from lipid microdomains, functioning as an inhibitor of insulin signaling and contributing to insulin resistance in adipocytes. Ganglioside GM3 mixture contains ganglioside GM3 molecular species with C18:1 and C20:1 fatty acyl chains.

Nitrated unsaturated fatty acids, such as 10- and 12-nitrolinoleate , cholesteryl nitrolinoleate, and nitrohydroxylinoleate, represent a new class of endogenous lipid-derived signalling molecules. LNO2 isomers serve as potent endogenous ligands for PPARγ and can also decompose or be metabolized to release nitric oxide. 9-Nitrooleate is one of two regioisomers of nitrooleate, the other being 10-nitrooleate (OA-NO2; used for the mixture of isomers), which are formed by nitration of oleic acid in approximately equal proportions in vivo. Peroxynitrite, acidified nitrite, and myeloperoxidase in the presence of H2O2 and nitrite, all mediate the nitration of oleic acid. OA-NO2 is found in human plasma as the free acid and esterified in phospholipids at concentrations of 619 ± 52 nM and 302 ± 369 nM, respectively. OA-NO2 activates PPARγ approximately 7-fold at a concentration of 1 μM and effectively promotes differentiation 3T3-L1 preadipocytes to adipocytes at 3 μM.

9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-conjugated linoleic acid reduces serum fasting glucose, insulin, and triglyceride levels and decreases white adipose tissue macrophage infiltration inob/obmice. It also increases body weight gain and body fat in weanling mice.4[Matreya, LLC. Catalog No. 1278] 1.Shultz, T.D., Chew, B.P., Seaman, W.R., et al.Inhibitory effect of conjugated dienoic derivatives of linoleic acid and β-carotene on the in vitro growth of human cancer cellsCancer Lett.63(2)125-133(1992) 2.Moya-Camarena, S.Y., Heuvel, J.P.V., Blanchard, S.G., et al.Conjugated linoleic acid is a potent naturally occurring ligand and activator of PPARαJ. Lipid Res.40(8)1426-1433(1999) 3.Moloney, F., Toomey, S., Noone, E., et al.Antidiabetic effects of cis-9, trans-11-conjugated linoleic acid may be mediated via anti-inflammatory effects in white adipose tissueDiabetes56(3)574-582(2007) 4.Pariza, M.W., Park, Y., and Cook, M.E.The biologically active isomers of conjugated linoleic acidProg. Lipid Res.40(4)283-298(2001)

Deacetylforskolin is a diterpene and a derivative of forskolin that has been found inC. forskohliiand has diverse biological activities.1,2,3,4It activates rat adipocyte adenylyl cyclase (IC50= 20 μM) and inhibits glucose transport in rat adipocyte plasma membranes.2Deactylforskolin (30-1,000 μg/kg) reduces blood pressure in spontaneously hypertensive rats.3It also attenuates hypercapnia-induced impairments in the passive avoidance response in mice.4 1.Gabetta, B., Zini, G., and Danieli, B.Minor Diterpenoids of Coleus forskohliiPhytochemistry28(3)859-862(1989) 2.Joost, H.G., Habberfield, A.D., Simpson, I.A., et al.Activation of adenylate cyclase and inhibition of glucose transport in rat adipocytes by forskolin analogues: structural determinants for distinct sites of actionMol. Pharmacol.33(4)449-453(1988) 3.Bhat, S.V., Dohadwalla, A.N., Bajwa, B.S., et al.The antihypertensive and positive inotropic diterpene forskolin: Effects of structural modifications on its activityJ. Med. Chem.26(4)486-492(1983) 4.McCulloch, A.J., Thomson, T.A., and Deacon, R.Hypoxic amnesia and its reversal with forskolinBiochem. Soc. Trans.17(1)212-213(1988)

Braco-19 is a telomerase/telomere inhibitor and an inhibitor of HAdV viral replication with antiviral activity that reduces lipid vacuolization in adipocytes, inhibits proliferation and decreases telomerase activity in human glioblastoma cells.

Pronuciferine ameliorate the glucose and lipid metabolism in insulin-resistant 3T3-L1 adipocytes.

Sparstolonin B, a selective TLR2 and TLR4 antagonist, is an isocoumarin compound isolated from the tubers of Sparganium stoloniferum and Scirpus yagara with anti-HIV, anticancer, antitumour and anti-inflammatory activities, inhibits selective Toll-like receptors, inhibits free fatty acids It inhibits selective Toll-like receptors, inhibits free fatty acid palmitate-induced chondrocyte inflammation and attenuates post-traumatic arthritis in obese mice, and inhibits lipopolysaccharide-induced inflammation in 3T3-L1 adipocytes, which can be used for validation and mammary carcinoma studies.

Secoisolariciresinol is an enterolignan precursor, it has antioxidant, and estrogen-like activities, it can significantly suppress triglyceride (TG) accumulation in 3T3-L1 adipocytes.

Spexin TFA, a potent agonist for galanin receptor 2/3 (GAL2/GAL3) with EC50 values of 45.7 and 112.2 nM respectively, shows no significant activity towards galanin receptor 1. As an endogenous peptide promoting satiety, it reduces long chain fatty acid uptake by adipocytes and lowers food consumption in diet-induced obese mice and rats. Additionally, it moderates LH secretion in goldfish and demonstrates anxiolytic effects in vivo.

S32826 is a highly potent inhibitor of autotaxin, exhibiting an IC50 value of 8.8 nM. It displays comparable inhibitory properties towards various autotaxin isoforms, including α, β, and γ. Furthermore, S32826 effectively inhibits the release of LPA from adipocytes.

Tibesaikosaponin V (TKV), a triterpene diglycoside isolated from the methanol extract of Bupleurum chinense DC roots, effectively inhibits lipid accumulation and triacylglycerol content in adipocytes without inducing cytotoxicity. It suppresses mRNA expression of nuclear transcription factors, including peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT/enhancer binding protein α (C/EBPα), and impedes 3T3-L1 preadipocyte differentiation. Considering these properties, Tibesaikosaponin V is a promising compound for researching obesity and related metabolic disorders [1].

MitoPQ (MitoParaquat) is a mitochondria-targeted small molecule compound that selectively enhances mitochondrial superoxide and hydrogen peroxide levels and inhibits insulin-stimulated glucose uptake and translocation of glucose transport protein 4 (GLUT4) to the plasma membrane in adipocytes and myotubes.MitoPQ can be used to MitoPQ can be used to study mitochondrial oxidative stress and regulated GLUT4 transporter.

Kihadanin B can repress the adipogenesis by decreasing lipid accumulation through the suppression of the Akt-FOXO1-PPARγ axis in 3T3-L1 adipocytes.

Agouti-related peptide (AgRP) is a neuropeptide produced in the brain by the AgRP/NPY neuron. It is only synthesized in NPY containing cell bodies located in the ventromedial part of the arcuate nucleus in the hypothalamus. The appetite-stimulating effect

Tert-OMe-byakangelicin is a coumarin known to potentiate adrenaline-induced lipolysis and impede insulin-mediated triglyceride synthesis from glucose in adipocytes [1].

NNMTi (5-Amino-1-methylquinolinium) is a substrate site-targeting, selective nicotinamide N-methyltransferase (NNMT) inhibitor (IC50 = 1.2 μM; 50 μM SAM, 100 μM NCA) that reduces 3T3-L1 lipogenesis (EC50 = 30μM) and adipocytes 1-methylnicotinamide level (EC50 = 2.3 μM) without affecting related methyltransferases & enzymes in the NAD+ salvage pathway

SSAO/VAP-1 Inhibitor 1 is a potent compound aimed at inhibiting SSAO/VAP-1, a protein involved in facilitating the translocation of Glucose Transport 4 (GLUT 4) to the cell membrane in adipocytes, thus playing a crucial role in glucose regulation. Additionally, in endothelial cells, this enzyme is responsible for mediating the adherence and infiltration of leukocytes, contributing to inflammatory responses. Given these mechanisms, SSAO/VAP-1 Inhibitor 1 holds considerable potential for research into treatments for inflammation, inflammation-related conditions, diabetes, and diabetes-associated diseases[1].

Ternatin is a cyclic heptapeptide first isolated from the mushroom C. versicolor that has been shown to have cytotoxic and anti-adipogenic effects in vitro. It inhibits adipogenesis with an IC50 value of 27 nM and becomes cytotoxic to 3T3-L1 mouse adipocytes at 10-fold higher concentrations. Ternatin is reported to inhibit HCT116 cell proliferation with an IC50 value of 71 nM. Note that this metabolite should not be confused with the plant flavonoid of the same name.

Endogenous APJ receptor agonist (EC50 = 20 nM) that is secreted by adipocytes. Binds with high affinity to human APJ receptors expressed in HEK 293 cells (pIC50= 8.61). Involved in regulation of cardiovascular function, fluid homeostasis and feeding. Bloc

Stearic acid-18,18,18-d3 is a deuterated compound of Stearic acid. Stearic acid has a CAS number of 57-11-4. 1. Stearic Acid can reduce metastatic tumor burden. 2. Stearic Acid leads to dramatically reduced visceral fat likely by causing the apoptosis of preadipocytes. 3. Stearic Acid and its derivatives have been used as gelators in food and pharmaceutical gel formulations. 4. Stearic Acid is a potent phosphatase 1B inhibitor, possibly causing an enhancement in the insulin receptor signaling to stimulate glucose uptake into adipocytes. 5. Stearic Acid has the potential to increase dry matter intake and yields of milk and milk components, without affecting conversion of feed to milk, body condition score, or body weight.

Sennidin B stimulates glucose incorporation in rat adipocytes.

Procyanidin B7, isolated from Solix sieboldiana, has been shown to mitigate mitochondrial defects in 3T3-L1 adipocytes induced by Dexamethasone. It enhances mitochondrial biogenesis, dynamics, transmembrane potential, and antioxidant defense to achieve this improvement.

(+)-Geodin is a fungal metabolite. It increases the fibrinolytic activity of bovine aortic endothelial cells (BAECs) when used at concentrations ranging from 50 to 150 μM. (+)-Geodin (1-100 μg/ml) also increases 2-deoxyglucose uptake by rat adipocytes.

Palmitoleic acid, an ω-7 monounsaturated fatty acid found in macadamia and sea buckthorn oils, enhances both basal and insulin-stimulated glucose uptake, as well as Glut4 protein levels in 3T3-L1 adipocytes at a 200 µM concentration. Ex vivo, at a dosage of 300 mg/kg per day, it significantly increases glucose uptake and both aerobic and anaerobic glycolysis, while decreasing de novo fatty acid synthesis and the activity of lipogenic enzymes, specifically ATP citrate lyase (ACL) and glucose-6-phosphate dehydrogenase (G6PDH), in isolated murine adipocytes. Furthermore, the dietary administration of palmitoleic acid at 300 mg/kg mitigates high-fat diet-induced insulin resistance and liver inflammation in mice.

IQZ23 is a chemical compound that effectively inhibits adipocyte differentiation by activating the AMPK pathway. It demonstrates high efficacy in reducing triglyceride levels (EC50=0.033 μM) in 3T3-L1 adipocytes. Given its properties, IQZ23 holds potential for research related to obesity and metabolic disorders.

Tachioside has antiobesity, antioxidant and α-glucosidase inhibitory activities, it decreases lipid content in 3T3-L1 adipocytes by inhibiting lipogenesis, shows antiobesity activities. Tachioside can inhibit nitric oxide production in lipopolysaccharides-stimulated RAW 264.7 cells with IC50 value of 12.14 μM.

Potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Exhibits no significant activity at galanin receptor 1. Endogenous satiety-inducing peptide; inhibits long chain fatty acid uptake by adipocytes and decreas

Amyloid A proteins (H2N-Ala-Gly-Leu-Pro-Glu-Lys-Tyr-OH) are a family of apolipoproteins associated with high-density lipoprotein in plasma. Different isoforms of SAA are expressed constitutively at different levels or in response to inflammatory stimuli.

Soyasaponin Aa and soyasaponin Ab dose-dependently markedly inhibit adipocyte differentiation and expression of various adipogenic marker genes, through the downregulation of the adipogenesis-related transcription factors PPARγ and C EBPα± in 3T3-L1 adipo

Endogenous APJ receptor agonist that is secreted by adipocytes. Binds with high affinity to APJ receptors (IC50 = 5.4 nM) and potently inhibits cAMP production in vitro (EC50 = 0.52 nM). Involved in regulation of cardiovascular function, fluid homeostasis

GPR81 agonist 1 is a potent and selective GPR81 agonist with high affinity for human and mouse GPR81, inhibiting lipolysis of differentiated 3T3-L1 adipocytes, improving insulin sensitivity and glycaemic control in mouse models of insulin resistance and diabetes, and can be used in the study of diabetes and obesity.