3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is a nucleotide analogue that inhibits DNA-dependent RNA polymerases I and II. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM[1].
Licochalcone D, a flavonoid compound mainly existing in the root of Glycyrrhiza inflate, is a potent inhibitor of NF-kappaB (NF-κB) p65. Licochalcone D possesses antioxidant, anti-inflammatory, anti-cancer properties[1][2].
Velneperit (S-2367) is a novel neuropeptide Y (NPY) Y5 receptor antagonist.Target: neuropeptide Y receptorVelneperit (S-2367) is a once-daily, oral, centrally acting, small molecule neuropeptide Y (NPY) Y5 receptor antagonist.
FFA3 agonist 1 (Compound 24) is an agonist of free fatty acid receptor 3 (FFA3). FFA3 agonist 1 regulates the health effect of intestinal microbiota by activating FFA3[1].
Borapetoside E can be isolated from T. crispa. Borapetoside E improves hyperglycemia, insulin resistance, hepatic steatosis, hyperlipidemia, and oxygen consumption in obese mice. Borapetoside E also inhibits SREBPs expression in the liver and adipose tissue[1].
Xanthine oxidoreductase-IN-3 is an orally active xanthine oxidoreductase (XOR) inhibitor, with an IC50 of 26.3 nM. Xanthine oxidoreductase-IN-3 can be used for the research of acute hyperuricemia[1].
Mogroside I E1, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities[1].
CP-775146 is a selective PPARα agonist that binds strongly to the PPARα ligand. CP-775146 efficiently alleviates obesity-induced liver damage, prevents lipid accumulation by activating the liver fatty acid β-oxidation pathway[1].
MK204 is an aldose reductase (AR) inhibitor that can be used in diabetes research[1].
Ganoderenic acid A is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid A is a potent inhibitor of β-glucuronidase. Ganoderenic acid A has a potent hepatoprotective effect against CCl4-induced liver injury[1].
Miglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose.Target: OthersMiglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose. It is primarily used in diabetes mellitus type 2 for establishing greater glycemic control by preventing the digestion of carbohydrates (such as disaccharides, oligosaccharides, and polysaccharides) into monosaccharides which can be absorbed by the body. Miglitol inhibits glycoside hydrolase enzymes called alpha-glucosidases. Since miglitol works by preventing digestion of carbohydrates, it lowers the degree of postprandial hyperglycemia. It must be taken at the start of main meals to have maximal effect. Its effect will depend on the amount of non-monosaccharide carbohydrates in a person's diet. Dietary supplementation with miglitol from pre-onset stage in OLETF rats delays the onset and development of diabetes and preserves the insulin secretory function of pancreatic islets [1]. Miglitol was orally administered at 40 mg/100 g of high-fat diet containing 45% kcal as fat to 12-week-old rats for 29 days, and age-matched rats without the agent were used as the respective controls [2].
p-Tolualdehyde-d7 is the deuterium labeled p-Tolualdehyde[1]. p-Tolualdehyde is an endogenous metabolite.
Ezetimibe phenoxy glucuronide-D4 (Ezetimibe glucuronide-D4) is the deuterium labeled Ezetimibe phenoxy glucuronide. Ezetimibe phenoxy glucuronide is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity[1]. Ezetimibe is a potent cholesterol absorption inhibitor[2].
Cystathionine-γ-lyase-IN-1 is a selective cystathionine γ-lyase (CSE) enzyme inhibitor with an IC50 of 6.3 μM[1].
Recaticimab (SHR-1209) is a humanized monoclonal antibody that inhibits PCSK9. Receticimab mediates the degradation of PCSK9 by binding to PCSK9, increasing the level of low-density lipoprotein (LDL) receptors on the surface of hepatocytes, reducing the level of LDL in plasma, and achieving the goal of lowering blood lipids. Recaticimab has potential application in hypercholesterolemia[1][2].
Oxyresveratrol 3'-O-β-D-glucopyranoside is a phenolic compound isolated from Morus nigra root and is an effective tyrosinase inhibitor with an IC50 of 1.64 μM[1].
Phytanic acid is an endogenous metabolite present in Blood that can be used for the research of Zellweger Syndrome, Alpha Methylacyl CoA Racemase Deficiency, Rhizomelic Chondrodysplasia Punctata and Infantile Refsum Disease[1][2][3][4][5].
MB07803 is an orally available prodrug of a potent, noncompetitive inhibitor (MB07729) of fructose 1,6-bisphosphatase (FBPase), with EC50 of 140 nM and t1/2 of 7.6±2.9 h.
7'-Hydroxy ABA (7'-OH ABA) is a metabolite of Abscisic acid (Abscisic acid) through hydroxylation of the 7′-carbon atom of Abscisic acid. 7'-Hydroxy ABA exhibits significant hormonal activity[1].
Aleglitazar(R1439; RO-0728804) is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.IC50 Value: 2.8 nM(PPAR-α); 4.6 nM(PPAR-γ)Target: PPARα/γAleglitazar (R1439) is a dual peroxisome proliferator-activated receptor (PPAR) agonist, with affinity to PPARα and PPARγ. Aleglitazar is being developed for the treatment of type II diabetes; It is currently in phase III clinical trials. In preliminary clinical studies, Aleglitazar has been demonstrated to improve hyperglycemia and dyslipidemia in patients with type 2 diabetes mellitus. Aleglitazar has beneficial effects on both lipid and glucose parameters and may have a therapeutic role in modifying cardiovascular risk factors and improving glycemic control in patients with T2DM. Aleglitazar combines the lipid benefits of fibrates and the insulin-sensitizing benefits of thiazolidinediones.
3, 4-seco-4 (23),20(29) -Lupadiene-3,28-dioic acid (Compound 5) is a triterpenoid compound. 3, 4-seco-4 (23),20(29)-Lupadiene-3,28-dioic acid has a strong inhibitory effect on the production of superoxide anions, and the inhibitory rate is 86.9±2.8% at 1 μM[1].
C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss[1][2][3][4][5].
Enuvaptan is a vasopressin receptor antagonist and has the potential for research into renal and cardiovascular diseases[1].
Sparfosic acid trisodium, is a potent inhibitor of aspartate transcarbamoyl transferase, with anti-tumor and antimetabolite activity. Aspartate transcarbamoyl transferase catalyzes the second step of de novo pyrimidine biosynthesis[1][2].
LYPLAL1-IN-1 (Compound 11) is an selective covalent small-molecule inhibitors of Lysophospholipase-like 1 (LYPLAL1) with an IC50 of 0.006 μM. LYPLAL1-IN-1 increases glucose production[1].
N-Octylmaleimide is an alkylmaleimide, which can inhibit rat liver glucose 6-phosphatase[1].
L-Histidine-13C6,d5,15N3 (H-His-OH-13C6,d5,15N3) hydrochloride hydrate is the deuterium, 13C-, and 15-labeled L-Histidine hydrochloride hydrate. L-Histidine hydrochloride hydrate (H-His-OH.HCl.H2O) is an endogenous metabolite.
THR-β agonist 5 (compound 54) is a potent THR-β agonist, with an EC50 of <50 nM[1].
Acetyl-Hirudin (54-65) (sulfated) binds directly to thrombin-rHCII(L444R) and disrupts interactions between the N-terminal acidic domain of rHCII and anion-binding exosite I of thrombin that serves to stabilize the complex[1].
Creatine D3 hydrate is a deuterium labeled Creatine hydrate. Creatine hydrate is pivotal in energy metabolism of muscle and brain cells, both in physiological and in pathological conditions[1].