GLP-1R agonist 13 (Compound 24) is a GLP-1 receptor agonist[1].
5-Hydroxylansoprazole (AG1908) is an active metabolite of Lansoprazole in plasma. Lansoprazole is metabolized by CYP2C19 forming 5-Hydroxylansoprazole. Lansoprazole is a gastric proton-pump inhibitor and is effective in the treatment of various peptic diseases[1][2].
Glicoricone, a phenolic compound, is isolated from a species of licorice. Glicoricone is an inhibitor of monoamine oxidase (MAO), with an IC50 of 140 μM. Glicoricone binds to estrogen receptor (ER) and shows estrogen antagonist activity[1][2].
Acanthopanaxoside A, a triterpenoid saponin, has pancreatic lipase inhibitory action[1].
Tenapanor (AZD1722) hydrochloride is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor hydrochloride reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor hydrochloride has the potential for the research of hyperphosphatemia[1][2].
Calcitriol D6 is the deuterated form of Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ), which is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).IC50 value:Target: vitamin D receptorCalcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) displays calcemic actions. Calcitriol stimulates intestinal and renal Ca2+ absorption and regulates bone Ca2+ turnover. Calcitriol (1,25-Dihydroxyvitamin D3; Rocaltrol )exhibits antitumor activity; Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) inhibits in vivo and in vitro cell proliferation in a wide range of cells including breast, prostate, colon, skin and brain carcinomas and myeloid leukemia cells.
AS1842856 is a potent and cell-permeable Foxo1 inhibitor with an IC50 of 30 nM.
FR-167356 is a potent, orally active and selective vacuolar ATPase inhibitor with IC50 values of 170, 220, 370, and 1200 nM for osteoclast plasma membranes, macrophage microsomes, renal brush border membranes, and liver lysosomal membranes, respectively. FR-167356 inhibits bone resorption and ovariectomy-induced bone loss[1].
URAT1 inhibitor 8 (example 247) is a potent URAT1 inhibitor, with an IC50 of 0.001 μM. URAT1 inhibitor 8 can be used for gout research[1].
Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
A novel potent, pan-AMPK activator with similar potency for all AMPK heterotrimers; increases the phosphorylation of the AMPK substrate ACC at S79 with EC50 of 121 nM, potently inhibits de novo lipogenesis (IC50=25 nM) in primary rat hepatocytes; increases PGC1a transcription and mitochondrial content, effectively activats AMPK in hepatocytes and in skeletal muscle; caused a rapid lowering of plasma glucose levels with no impact on hepatic glucose production in diabetic mice.
FF-MAS is a potent meiotic maturation agonist. FF-MAS promotes meiotic maturation and preimplantation development of mouse oocytes maturing in vitro. FF-MAS promotes the completion of meiotic maturation to metaphase II (MII) and improves competence to complete the 2-cell stage to blastocyst transition[1][2].
AU-224 is a benzamide derivative used as a promising gastrointestinal prokinetic agent without significant side effects.
L6H21, a derivative of chalcone, is an orally active and potent MD-2 (myeloid differentiation factor 2) inhibitor. L6H21 inhibits TLR4-NF-κB signaling and NLRP3 inflammasome activation in macrophages. L6H21 inhibits EtOH + LPS-induced apoptosis and mitochondrial damage in RAW264.7 cells. L6H21 effectively inhibits EtOH + LPS-induced hepatic fat accumulation and liver injury. L6H21 shows neuroprotective effect in a model of prediabetes[1][2].
GDP-L-fucose disodium is a nucleotide sugar that is a key substrate for the biosynthesis of fucose oligosaccharides. GDP-L-fucose disodium provides the fucose moiety for the oligosaccharides. The formation of GDP-L-fucose disodium occurs through two pathways, the major de novo metabolic pathway and the minor remedial metabolic pathway[1].
YW1128 is an inhibitor of Wnt/��-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.
(R)-Monlunabant ((R)-MRI-1891) is a CB1 receptor mediators for research of obesity and metabolic disease[1]
Oct-1-en-3-ol, a fatty acid fragrant, is a self-stimulating oxylipin messenger. Oct-1-en-3-ol serves as a signaling molecule in plant cellular responses, plant-herbivore interactions, and plant-plant interactions. Oct-1-en-3-ol causes dopamine neuron degeneration through disruption of dopamine handling[1][2].
WS-12 is an agonist of TRPM8 with an EC50 of 39 nM.
Bombesin is a tetradecapeptide originally isolated from frog skin; plays an important role in the release of gastrin and the activation of G-protein receptors.
Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist. Resomelagon induces ERK1/2 phosphorylation and Ca2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research[1][2].
4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a Ki of 12 mM for wild-type 2-deoxy-D-glucose transport[1][2][3].
BYK 191023 is a highly selective inducible nitric-oxide synthase (iNOS) inhibitor. BYK 191023 interacts with the catalytic center of the enzyme. BYK 191023 can be used to study the in vivo and in vitro effects mediated by iNOS [1].
SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
Gancaonin L is an isoflavone, that can be isolated from Glycyrrhiza glabra roots. Gancaonin L exhibits significant PPAR-γ ligand-binding activity. Gancaonin L can be used for anti-diabetes and anti-obesity research[1].
(R)-Pantetheine is the biosynthetic precursor to CoA.(R)-Pantetheine and its corresponding disulfide pantethine, play a key role in metabolism as a building block of coenzyme A (CoA)[1].
Indole-3-methanamine is a potential biomarker for the consumption of these foods such as barley, cereals, and cereal product[1].
5-Methyltetrahydrofolic acid is a biologically active form of folic acid. 5-Methyltetrahydrofolic acid is a methylated derivate of tetrahydrofolate. 5-Methyltetrahydrofolic acid is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid[1].
Mildronate dihydrate (Meldonium dihydrate) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC50 values of 34-62 μM for human recombinant BBOX and an EC50 of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes[1].
Enterostatin, human, mouse, rat is a pentapeptide that reduces fat intake.