anti-metabolic

3,5,7,3′,4′-Pentamethoxyflavone (Quercetin 3,5,7,3,4-pentamethyl ether) is a natural product that induces adipogenesis in 3T3-L1 preadipocytes by regulating transcription factors during the early stages of differentiation.

GW9662 (TIMTEC-BB SBB006523) is a PPARγ antagonist (IC50=3.3 nM) with selectivity. GW9662 can be used to study the pathogenesis of metabolic diseases, such as obesity and diabetes, by inhibiting the activity of PPARγ. GW9662 can be used to study the pathogenesis of inflammatory diseases, such as atherosclerosis and rheumatoid arthritis. GW9662 has anti-tumor effect.

Tiludronate disodium (Tiludronic acid disodium) is an osteoclast vacuolar H(+)-ATPase inhibitor with antiresorptive and anti-inflammatory properties. Tiludronate disodium can be used in studies about metabolic bone disorders.

Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss.

L-DOPA (Levodopa) is an orally active metabolic precursor of the neurotransmitter dopamine. It can cross the blood-brain barrier and be converted into dopamine in the brain. L-DOPA exhibits anti-hyperalgesic effects and holds potential in Parkinson’s disease research, and it can also be used to induce Parkinson’s disease models.

Betamethasone valerate (Luxiq) is a synthetic glucocorticoid with metabolic, immunosuppressive and anti-inflammatory actions.

Rofecoxib (MK 966) binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in an inhibition of the conversion of arachidonic acid to prostaglandins. Rofecoxib is a synthetic, nonsteroidal derivative of phenyl-furanone with anti-inflammatory, antipyretic and analgesic properties and potential antineoplastic properties. COX-related metabolic pathways may represent key regulators of cell proliferation and neo-angiogenesis. Some epithelial tumor cell types overexpress pro-angiogenic COX-2.

AICAR (Acadesine) is an AMPK activator. AICAR has the functions of metabolic regulation, muscle function regulation, anti-cancer effect, neuroprotection and anti-aging.

Betamethasone Dipropionate is the 17, 21-dipropionate ester of betamethasone, a synthetic glucocorticoid with metabolic, immunosuppressive and anti-inflammatory actions. Betamethasone dipropionate (SCH 11460) binds to specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. The synthesis of certain anti-inflammatory proteins is induced while the synthesis of certain inflammatory mediators is inhibited. As a result, there is an overall reduction in chronic inflammation and autoimmune reactions.

1,3-Dithiane (1,3-Dithian) is a protected formaldehyde anion equivalent that could serve as a useful labeled synthon. 1,3-Dithiane is also a sulfur-containing Maillard reaction products found in boiled beef extracts.

Emodin (Frangula emodin) is an 11β-HSD1 inhibitor with a selective IC50 of 186 and 86 nM against 11β-HSD1 in humans and mice, respectively. Emodin has antiviral, anti-inflammatory, and anti-cancer effects. Emodin can improve metabolic disorders in diet-induced obese mice.

Lycorine (Narcissine) inhibits protein synthesis and may inhibit ascorbic acid biosynthesis, although studies on the latter are controversial and inconclusive.

Glabridin (KB-289522) may serve as an anti-inflammatory agent in diabetes-related vascular dysfunction, through regulating the synthesis and activity of iNOS under high-glucose levels; may possess a therapeutic effect on metabolic disorders( such as diabetes and hyperglycemia), by modulating glucose metabolism through AMPK in skeletal muscle cells. Glabridin may have potential as a chemopreventive agent against liver Y metastasis, by inhibiting the invasion of human HCC cells.

Spirorenone (INN) is a novel aldosterone antagonist with anti-salt corticosteroid activity, used in metabolic disease research.

AZ12216052 is a GRP8 antagonist with anxiolytic and anti-inflammatory activity and can be used to study obesity and metabolic disorders.

LDCA is a double-hit metabolic regulator that exhibits potent anti-proliferative activity. lDCA competitively inhibits LDH-A enzyme activity, alters mitochondrial hyperpolarization and simultaneously subverts apoptosis. lDCA has a pronounced effect in cancer cells and does not show toxicity.

Medrysone (6α-Methyl-11β-hydroxyprogesterone) is a topical, synthetic glucocorticoid with metabolic, anti-inflammatory and anti-allergic properties. Medrysone exerts its effect by interacting with specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. This results in an induction of the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Consequently, an overall reduction in chronic inflammation and autoimmune reactions is accomplished.

DB1976 dihydrochloride (DB1976 2HCl) , a transcription factor PU.1 inhibitor with potential anti-inflammatory activity, slowed down inflammation and fibrosis and improved glucose homeostasis and dyslipidemia in mice in in vivo experiments.DB1976 dihydrochloride promotes apoptosis and may be used in studies of metabolic dysfunction and non-alcoholic steatohepatitis.

Enzalutamide-d3 (Deutenzalutamide-d3) is a deuterium-labeled form of the androgen receptor antagonist enzalutamide, retaining potent anti-androgen and antineoplastic activity with an IC50 of 36 nM in LNCaP prostate cancer cells, and is primarily used in pharmacokinetic, metabolic tracing, and drug interaction studies.

Setmelanotide (RM-493) is a selective melanocortin-4 receptor agonist with EC50 values of 0.27 and 0.28 nM for human and rat MC4R. Setmelanotide enhances cAMP signaling, demonstrates functional selectivity, activates sympathetic preganglionic neurons to influence blood pressure, and is widely used to probe MC4R-MRAP2 interactions. Setmelanotide contributes to obesity-related research by modulating hunger and satiety circuits, reversing risperidone-induced weight gain in mice, and helping characterize MC4R variants in pediatric metabolic disorders. The anti-inflammatory actions of Setmelanotide in astrocytoma cells and the utility in combination with calorie restriction further highlight its broad value in metabolic and neuroendocrine research.

Alternariol is a natural product extracted from Etoac that demonstrates anti-inflammatory activity in vitro and in vivo in murine hepatoma cells and in human serum, with additional effects on toll-like receptor signaling and regulation of pro-apoptotic protein expression. Alternariol has been shown to be inactive against methyl transferase enzymes, a feature relevant to its metabolic inactivation profile.

RIPK1-IN-26 is a potent inhibitor of Receptor-Interacting Serine/Threonine Kinase 1 (RIPK1), exhibiting anti-necrotic properties in cells. This compound demonstrates good metabolic stability and binding specificity in mice. RIPK1-IN-26 holds potential for development as a PET imaging probe and in the research of neurodegenerative diseases.

PT109 is a multikinase inhibitor that targets JNK and other kinases, playing a crucial role in anti-inflammatory, antioxidative, neurogenic, and synaptogenic processes. Specifically, PT109 inhibits JNK isoforms with the following IC50 values: JNK1 at 0.143 μM, JNK2 at 0.831 μM, and JNK3 at 0.285 μM. It also inhibits SGK isoforms (SGK1: IC50=1.34 μM; SGK2: IC50=5.6 μM; SGK3: IC50=26.4 μM) and ROCK2 (IC50=34 μM). Additionally, PT109 reprograms polymorphic glioblastoma multiforme (GBM) into oligodendroglia via the PTBP1/PKM1/2 pathway and alters the metabolic pattern of GBM to exhibit antiglioma activity.

FKK6 is a selective agonist of the pregnane X receptor (PXR) with an EC50 of 1.2 µM. It demonstrates strong affinity for plasma proteins and exhibits favorable metabolic characteristics in human microsomes. FKK6 inhibits the PXR-related NF-κB signaling pathway, reducing the expression of inflammatory factors and showing anti-inflammatory activity in a mouse model of DSS-induced colitis.