hfd

MTHFD2-IN-3 (compound 10), a potent inhibitor of methylenetetrahydrofolate dehydrogenase (MTHFD2), demonstrates significant efficacy in obstructing the activity of this enzyme [1].

MTHFD2-IN-4, a tricyclic coumarin derivative, serves as a potent inhibitor of MTHFD2 and has applications in cancer research [1].

MTHFD2-IN-1 (compound 12) is a potent inhibitor of methylenetetrahydrofolate dehydrogenase (MTHFD2) [1].

MTHFD2-IN-4 sodium, a potent inhibitor of MTHFD2 and a tricyclic coumarin derivative, is applicable in cancer research [1].

MTHFD2-IN-2 (compound 13) is a potent inhibitor of methylenetetrahydrofolate dehydrogenase (MTHFD2) [1].

MTHFD2-IN-5 (Compound 16e) is a selective inhibitor of MTHFD2 with an IC50 of 66 nM. It inhibits the proliferation of MOLM-14 cells with a GI50 of 720 nM and demonstrates antitumor activity in mouse models.

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.

SBC-115076 is a potent extracellular proprotein convertase subtilisin kexin type 9 (PCSK9) antagonist.

Lansoprazole (A-65006) is a 2, 2, 2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

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

BVT 2733 is a new, non-steroidal, isoform-specific inhibitor of 11β-HSD1.

Serpentine is an alkaloid found in the roots of Rosa Centifolia that acts as an insulin sensitizer to assist insulin in lowering blood glucose.Serpentine activates the phosphorylation of AMPK, which stimulates glucose uptake by C2C12 cells.Serpentine increases the expression of GSK-3β mRNA in muscle tissues, which enhances glucose uptake.Serpentine also increases glucose production and hepatic gluconeogenesis.Serpentine has a significant effect on glucagon secretion and hepatic gluconeogenesis. Serpentine significantly increased glucagon secretion and hepatic gluconeogenesis. In high-fat diet streptozotocin (HFD STZ)-induced diabetic mice, Serpentine significantly prolonged insulin hypoglycemia, significantly decreased exogenous insulin use, and inhibited endogenous insulin secretion.

A3051, is a robust and orally active inhibitor of CXXC5-DVL with an IC 50 of 63.06 nM. Its applications include research into phenotypes associated with obesity, diabetes, and NASH that are induced by high fat diet (HFD) and methionine-choline deficient diet (MCD).

INF200 (compound 5), a sulfonylurea-based inhibitor of NLRP3 and associated pyroptosis, exhibits cardiometabolic benefits in a rat model of high-fat diet (HFD)-induced metaflammation and demonstrates anti-inflammatory effects by reducing IL-1β release in human macrophages at a concentration of 10 μM. Additionally, it enhances glucose and lipid profiles, diminishes systemic inflammation and cardiac dysfunction biomarkers, notably BNP, and ameliorates myocardial damage linked to ischemia reperfusion injury (IRI) as assessed by hemodynamic parameters [1].

KPLH1130, a specific pyruvate dehydrogenase kinase (PDK) inhibitor, enhances glucose tolerance in mice fed a high-fat diet (HFD). It effectively hinders macrophage polarization and mitigates proinflammatory reactions.

KY19382 (2H-Indol-2-one, 5,6-dichloro-3-[1,3-dihydro-3-(methoxyimino)-2H-indol-2-ylidene]-1,3-dihydro-Ky19382) is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β( IC50s of 19 and 10 nM, respectively). It activates Wnt β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.

PTUPB is a potent dual inhibitor of sEH and COX-2 enzymes with IC50 values of 0.9 nM and 1.26 μM, respectively.

Mahanimbine is found in the roots, leaves and stems of Murraya koenigii and is an orally active alkaloid extracted from Murraya koenigii. Bifidobacterium bifidum leaves on histopathological changes in pancreatic beta cells of streptozotocin-induced diabetic rats.

ACH-000143 have been identified as a novel agonist of the melatonin receptors MT1 and MT2.

Lipid-lowering agent-2 (Compound 14d) exhibits oral efficacy as a lipid-lowering agent with an EC50 of 0.06 μM. It works by inhibiting lipid synthesis and activating the AMPK signaling pathway, contributing to its anti-obesity effects. Additionally, Lipid-lowering agent-2 suppresses food intake in mice, enhances glucose metabolism, and reduces body weight and adipose tissue in mice induced by a high-fat diet (HFD).

FXR agonist9 (compound 26) is a selective, orally active partial agonist of FXR with an EC50 of 0.09 µM (maximum efficacy of 75.13%). It ameliorates the pathological features of fatty liver disease in mice induced by HFD and CCl4-related metabolic dysfunction.

Ficusin has antioxidant, antilipidemic and antidiabetic effects, it can lower the levels of fasting blood glucose, plasma insulin, body weight gain in HFD-STZ induced diabetic rats, and can significantly enhance the PPARγ expression and improve the transl

ATF3 inducer 1 is an efficient ATF3 inducer with lipid-lowering and anti-hyperglycemic activities. It alleviates glucose intolerance and insulin resistance induced by high-fat diet (HFD) and ameliorates liver steatosis induced by HFD. It can be used for research on obesity.

Asperlin is an orally active marine-derived antibiotic with antifungal, anticancer, anti-inflammatory, and anti-atherosclerotic properties. It can induce apoptosis and increase reactive oxygen species (ROS) and DNA damage-related G2 M phase arrest, as well as ATM phosphorylation. Additionally, Asperlin effectively prevents HFD-induced obesity in vivo and modulates gut microbiota.