Metadoxine blocks adipocyte differentiation in association with inhibition of the protein kinase A-cAMP response element binding protein (PKA-CREB) pathway.
[Tyr4]-Bombesin is a Bombesin analogue, is a ligand of gastrin-releasing peptide receptor (GRPR)[1].
Stearic acid-1-13C is the 13C labeled Stearic acid. Stearic acid is a long chain dietary saturated fatty acid which exists in many animal and vegetable fats and oils.
Glycolate oxidase-IN-1(compound 26), a salicylic acid derivative, is a glycolate oxidase (GO) inhibitor with an IC50 of 38.2 μM. Glycolate oxidase-IN-1 has the ability to reduce oxalate production in hyperoxalate hepatocytes and can be used in the study of primary hyperoxaluria type 1 (PH1)[1].
Tigulixostat is a novel (indolyl)heteroarylcarboxylate derivatives effective as non-purine selective xanthine oxidase inhibitor, which lowers the production of uric acid[1].
HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, and 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake[1].
GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
UDP-Galactose is a monosaccharide involved in nucleotide sugar metabolism. UDP-Galactose and its derivatives act as a natural agonist for Gi protein-conjugated P2Y14 receptors in the immune system (IC50=0.67 μM, hP2Y14)[1].
Rimonabant(SR141716) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.IC50 Value: 1.8 nM(Ki)Target: CB1 Receptorin vitro: Rimonabant dose-dependently reduces ACAT activity in Raw264.7macrophages with IC50 of 2.9 μM and isolated peritoneal macrophages. Rimonabant inhibits ACATactivity in intact CHO-ACAT1 and CHO-ACAT2 cells and in cell-free assays with approximately equal efficiency with IC50 of 1.5 μM and 2.2 μM for CHO-ACAT1 and CHO-ACAT2, respectively. Consistent with ACAT inhibition, Rimonabant treatment blocks ACAT dependent processes in macrophages, oxysterol-induced apoptosis and acetylated-LDL induced foam cell formation. Rimonabant antagonizes the inhibitory effects of cannabinoid receptor agonists on both mouse vas deferens contractions and adenylyl cyclase activity in rat brain membranes in a concentration-dependent manner.in vivo: Rimonabant (10 mg/kg by gavage) is fed for 2 weeks to 3-month-old male obese Zucker rats as an impaired glucose tolerance model and for 10 weeks to 6-month-old male obese Zucker rats as a model of the metabolic syndrome. RANTES (Regulated upon Activation, Normal T cell Expressed, and Secreted) and MCP-1 (monocyte chemotactic protein-1) serum levels are increased in obese vs lean Zucker rats and significantly reduced by long-term treatment with Rimonabant, which slowes weight gain in rats with the metabolic syndrome. Neutrophils and monocytes are significantly increased in young and old obese vs lean Zucker rats and lowered by Rimonabant. Platelet-bound fibrinogen is significantly enhanced in obese vs lean Zucker rats of both age, and is reduced by Rimonabant. Platelets from obese rats are more sensitive to thrombin-induced aggregation and adhesion to fibrinogen, which are both attenuated by Rimonabant therapy.
4,7-Didehydroneophysalin B is a flavonoid with cholinesterase inhibiting activity. 4,7-Didehydroneophysalin B can be isolated and purified from the natural Physalis alkekengi L. var. franchetii (Mast.) Makino.
Linagliptin-13C,d3 is the 13C- and deuterium labeled. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
Robustaflavone is a biflavonoid isolated from Doradilla that has natriuretic properties[1].
Mead acid (5,8,11-Eicosatrienoic acid), an unsaturated (Omega-9) fatty acid, is an indicator of essential fatty acid deficiency[1].
Cognac oil, mainly found in wine lees, has unique fatty acid profiles, including Palmitic acid (59.26%), Linoleic acid (11.92%), Myristic acid (8.97%), Oleic acid (8.3%) and other fatty acids. Cognac oil leads to a general increase in the permeation of R6G (Rhodamine 6G) across all the membranes[1].
L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a Ki of 63 nM[1][2].
L-Arabinitol is a potential biomarker for the comsuption of the food products such as sweet potato, deerberry, moth bean, and is also associated with Alzheimer's disease and ribose-5-phosphate isomerase deficiency.
Pancreastatin (37-52), human is a pancreastatin fragment. Pancreastatin a CgA-derived peptide (CgA residues 250–301) with biological activity, inhibited the releasing of insulin by islet beta cells[1][2].
Adenosine-2′-13C is the 13C labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiolo
Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol. Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities[1].
1-Dehydroxybaccatin IV is a taxane diterpene. 1-Dehydroxybaccatin IV shows concentration-dependent NO inhibition, with an IC50 of 32.2 μM[1].
SB-423557 is an orally active calcium-sensing receptor (CaR) antagonist (IC50=520 nM), precursor of SB-423562 (IC50=73 nM). SB-423557 is well tolerated in human and increases plasma concentrations of exogenous parathyroid hormone (PTH) and stimulates bone formation[1].
Ac-Asp-Tyr(PO3H2)-Val-Pro-Met-Leu-NH2 is the SH2 domain ligand. SH2 domains participate in protein tyrosine kinase (PTK)-mediated cellular signal[1].
BBT is an enhancer of impaired glucose-stimulated insulin secretion (GSIS). BBT exhibits anti-hyperglycemia activity, and protects β-cells from cytokine- or streptozotocin (STZ)-induced cell death in type 2 diabetes models. BBT acts function via cAMP/PKA and long-lasting (L-type) voltage-dependent Ca2+ channel/CaMK2 pathway[1].
FR194738 free base is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
URAT1 inhibitor 4, a Lesinurad derivative, is a potent and orally active URAT1 inhibitor with an IC50 of 7.56 μM. URAT1 inhibitor 4 has higher in vivo urate-lowering efficacy than Lesinurad (HY-15258)[1].
GI 181771 is a cholecystokinin 1 receptor agonist investigated for the treatment of obesity.
H-HoPro-OH is a breakdown product of lysine, accumulates in body fluids of infants with generalized genetic peroxisomal disorders, such as Zellweger syndrome, neonatal adrenoleukodystrophy.
Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into the cell in vivo. Tributyrin has potent antiproliferative, proapoptotic and differentiation-inducing effects[1].
3-Hydroxybutyric acid-d2 (sodium) is the deuterium labeled 3-Hydroxybutyric acid sodium[1]. 3-Hydroxybutyric acid sodium (β-Hydroxybutyric acid sodium) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid sodium can modulate the properties of membrane lipids[2].
Obestatin(11-23)mouse, rat is a polypeptide involved in regulating energy balance and inhibiting eating. Obestatin(11-23)mouse, rat causes reduced food intake, body weight, and jejunal contractions in rodents[1].