adipocytes

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

Avicularin (Fenicularin) has anti-allergic, anti-inflammatory, hepatoprotective, antioxidant, anti-tumor and other activities. It ameliorates human hepatocellular carcinoma by modulating the activities of NF-κB(p65), COX-2, and PPAR-γ. In LPS-stimulated RAW 264.7 macrophages, it exerts anti-inflammatory activity by inhibiting the ERK signaling pathway.

Kudinoside D exerts anti-adipogenic effects through modulation of adipogenic transcription factors via AMPK signaling pathway.

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.

Methyl cinnamate, a tyrosinase inhibitor and a flavoring compound, has antimicrobial, antiadipogenic, vasorelaxant, and anti-inflammatory effects.

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.

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.

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.

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.

IBC 293 is selective for GPR109B over niacin receptor GPR109A. IBC 293 is a highly selective agonist for GPR109B, a human orphan G-protein-coupled receptor expressed in adipocytes.

LG100268 is a potent, selective, and orally active retinoid X receptor (RXR) agonist that agonizes RXR-α, RXR-β, and RXR-γ at the nanomolar level, selectively exceeding the RAR by three orders of magnitude.LG100268 is capable of inducing transcriptional activation in adipocytes; affecting the RXRs and their chaperone receptor, Foxl2/Dmrt1, to induce flounder masculinization in juvenile flounder; inhibits keratin 17 expression in nigrostriatal epithelial cells; and increases PD-L1 expression in HER2 or triple-negative breast cancer.

CXM102 is an activator of autophagy. This compound induces autophagy in aged BMSCs, rejuvenating them and promoting their preferential differentiation into osteoblasts. CXM102 enhances the nuclear translocation of transcription factor EB (TFEB) and the formation of osteoblasts. In middle-aged male mice, it stimulates bone anabolic metabolism, reduces marrow adipocytes, delays bone loss, lowers serum inflammation levels, reduces organ fibrosis, and extends lifespan.

Wnt/β-catenin activator 1 (Compound 5m) is an orally active activator of the Wnt/β-catenin signaling pathway. It induces cell cycle arrest in the G1 phase, inhibits early proliferation of adipocytes, and suppresses adipogenesis in 3T3-L1 cells with an IC50 of 330 nM. In a high-fat diet-fed Syrian golden hamster model, Wnt/β-catenin activator 1 exhibits anti-adipogenic and anti-dyslipidemic activities.

AMPK activator17 (Compound 10g) is an orally bioavailable AMPK activator. It significantly inhibits lipogenesis (IC50: 3.4 μM) and improves dyslipidemia. By activating the AMPK pathway, AMPK activator17 suppresses early adipocyte differentiation (mitotic clonal expansion) and enhances mitochondrial function and fatty acid oxidation in mature adipocytes. It improves dyslipidemia through promoting cholesterol reverse transport. AMPK activator17 is applicable in research on obesity and associated metabolic disorders, such as type 2 diabetes and cardiovascular diseases.

ZGL-18 is a mitochondrial uncoupler inspired by uncoupling protein 1 (UCP1). It activates brown adipocytes and reduces mitochondrial membrane potential.

Sulfosuccinimidyl myristate sodium is an inhibitor of fatty acid transport. In isolated rat adipocytes, it effectively suppresses the uptake of [14C]stearate.

Galegine hemisulfate, a guanidine derivative, aids in weight reduction in mice. It activates AMPK in 3T3-L1 adipocytes, L6 myotubes, H4IIE rat hepatoma cells, and HEK293 human renal cell lines. Galegine hemisulfate also exhibits antibacterial activity, with a minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains.

15-Deoxy-Δ12,14-Prostaglandin J2-2-glyceryl ester is a derivative of 15-Deoxy-Δ-12,14-prostaglandin J2. The 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. This compound acts as a selective PPARγ (with an EC50 of 2 µM) and covalent PPARδ agonist. Additionally, 15-Deoxy-Δ-12,14-prostaglandin J2 effectively promotes the differentiation of C3H10T1/2 fibroblasts into adipocytes, with an EC50 of 7 μM.

RG-239 is an orally active TGR5 agonist with an EC50 of 120 nM, significantly more potent than Betulinic acid (EC50= 1.04 μM). It exhibits much higher selectivity for TGR5 over FXRα. The compound enhances mitochondrial activity in adipocytes and promotes neurite outgrowth at higher concentrations. Additionally, RG-239 inhibits LPS-induced iNOS expression and nitrite production in Raw264.7 cells and microglia. RG-239 is applicable for research related to type 2 diabetes.

NR4A1 agonist 1 is an NR4A1 agonist with a Ki value of 2.96 μM. It demonstrates significant lipid-lowering activity in 3T3-L1 adipocytes, with an EC50 of 0.13 μM, effectively reducing triglyceride (TG) accumulation and lipid droplet formation. NR4A1 agonist 1 is applicable in obesity-related research.

PPARγagonist-22 is a PPARγ agonist that enhances glucose uptake by cells and reduces lipid accumulation in adipocytes. It is useful for research related to type 2 diabetes.

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

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.

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.