Kaempferol 3-O-gentiobioside is a flavonoid isolated from C. alata leaves with antidiabetic activity. Kaempferol 3-O-gentiobioside possesses activity against α-glucosidase and displays carbohydrate enzyme inhibitory effect with an IC50 of 50.0 µM[1].
ABC34 is an inactive control compound of JJH260. ABC34 does not inhibit the fluorophosphonate reactivity or fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1. ABC34 can inhibit both ABHD6 and PPT122[1].
VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM[1].
Strontium ranelate(S12911) stimulates the calcium sensing receptors (CaSR) and leads to the differentiation of pre-osteoblast to osteoblast which increases the bone formation.IC50 value:Target: CaSRStrontium Ranelate is a bone metabolism modulator that inhibits bone resorption while maintaining bone formation. Strontium Ranelate acts by increasing bone formation and decreasing bone resorption, thus rebalancing bone turnover in favour of bone formation, an effect that results in increased bone mass and strength. Commonly used as an antiosteoporotic. Strontium Ranelate has shown efficacy in preventing early postmenopausal bone loss and reducing the risk of hip fracture in women with postmenopausal osteoporosis.
Quercetin 3-O-(6''-O-malonyl)-β-D-glucoside, a natural flavonol glycoside, possesses antioxidant activity[1].
Lipase Substrate is a substrate of lipase to detect activity[1].
Uridine diphosphate glucuronic acid (UDP-GlcA) ammonium is a cofactor that is formed by the catalytic activity of UDP-glucose dehydrogenase. Uridine diphosphate glucuronic acid (ammonium) is a central precursor in sugar nucleotide biosynthesis and common substrate for C4-epimerases and decarboxylases releasing UDP-galacturonic acid (UDP-GalA) and UDP-pentose products, respectively. Uridine diphosphate glucuronic acid (ammonium), as a glucuronic acid donor, can be used for for the research of the conjugation of bilirubin in the endoplasmic recticulum[1].
YM543 free base is a potent and orally active sodium-glucose cotransporter (SGLT) 2 inhibitor. YM543 free base reduces blood glucose levels. YM543 free base can be used in research of diabetes[1][2].
Velaglucerase alfa is produced through gene activation technology and is identical to wild-type enzyme. Velaglucerase alfa targets accumulated glucocerebroside primarily within the lysosome of the macrophages in the affected organs and systems. Velaglucerase alfa is an enzyme replacement therapy (ERT) for type 1 Gaucher disease (GD)[1].
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor.
L-Glutamic γ-monohydroxamate is an antitumor agent, inhibits cell proliferation. L-Glutamic γ-monohydroxamate selectively inhibits the uptake of L-histidine into microvascular endothelial cell. L-Glutamic γ-monohydroxamate, as a vanadium ligand, activates glucose uptake and metabolism, thus decreases the blood glucose levels in vivo[1][2][3].
VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM).IC50 value: 1 nM (trypsin-like proteasome), 50-100 nM(chymotrypsin-like proteasome), 3 μM (caspase-like proteasome)Target: proteasomein vitro: VR23 is a novel proteasome inhibitor targeting β2 of the 20S proteasome subunit. VR23 produces a synergistic effect in killing multiple myeloma cells, including those that were resistant to bortezomib. VR23 as a structurally novel proteasome inhibitor with desirable properties as an anticancer agent.in vivo: VR23 shows effective antitumor and antiangiogenic activities in mice.
D-Alanyl-L-leucine (D-Ala-Leu) is a dipeptide that acts as a source donor of L-Leucine (HY-N0486)[1].
H-Hyp-Gly-OH is a dipeptide containing hydroxyproline and glycine. H-Hyp-Gly-OH promotes the growth of mouse primary fibroblasts on collagen gel. H-Hyp-Gly-OH has potential applications in improving skin by ingesting hydrolyzed collagen. H-Hyp-Gly-OH can be used for metabolic research[1].
AA26-9 is a potent and broad spectrum serine hydrolase inhibitor.
(-)-Hydroxycitric acid lactone (Garcinia lactone) is an anti-obesity agent and a popular weight loss food supplement. (-)-Hydroxycitric acid lactone is a potent inhibitor of ATP-citrate lyase. (-)-Hydroxycitric acid lactone catalyzes the extramitochondrial cleavage of citrate to oxaloacetate and acetyl-CoA, limits the availability of acetyl-CoA units required for fatty acid synthesis[1][2].
BX341 is an anti-androgen.
Ac-D-DGla-LI-Cha-C is a potent HCV protease inhibitor peptide. Ac-D-DGla-LI-Cha-C can be used for the research of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases[1].
Hippuric Acid, an acyl glycine produced by the conjugation of benzoic acid and glycine, is a normal component in urine as a metabolite of aromatic compounds from food.
2-Deoxy-D-glucose 6-phosphate disodium, a derivative of 2-Deoxy-D-glucose, is produced in mammalian cells by the action of hexokinase on 2-DG. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1].
TFAP is a selective cyclooxygenase-1 (COX-1) inhibitor, with an IC50 of 0.8 μM.
ER proteostasis regulator-1 (compound 481) is a potent ER proteostasis regulator. ER proteostasis regulator-1 has the potential for the research of Alzheimer's disease and diabetes[1].
Fructosyl amino acid oxidase can be used to measure glycosylated protein. Glycosylated protein, especially glycosylated hemoglobin A1c, is an important marker to evaluate the efficacy of diabetes treatment[1].
Spironolactone is a potent antagonist of the androgen receptor. Target: Androgen ReceptorSpironolactone is a potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. 5% topical spironolactone cream acts as an antiandrogen in human sebaceous glands, competing with DHT receptors and producing a decrease of labelled DHT. At the concentrations used the effect has been only local. No side-effects were recorded during both studies [1]. Patients who received spironolactone had a significant improvement in the symptoms of heart failure, as assessed on the basis of the New York Heart Association functional class (P<0.001). Gynecomastia or breast pain was reported in 10 percent of men who were treated with spironolactone, as compared with 1 percent of men in the placebo group (P<0.001). The incidence of serious hyperkalemia was minimal in both groups of patients [2].
Uridine 5'-diphosphate sodium salt is a potent, selective P2Y6 receptor native agonist (EC50=300 nM; pEC50=6.52) and a potent P2Y14 antagonist (pEC50=7.28). Uridine 5'-diphosphate sodium salt, an endogenous metabolite, catalyzes the glucuronidation of a wide array of substrates and is used in nucleic acid (RNA) biosynthesis[1][2].
Vanin-1-IN-2 is a potent vanin-1 inhibitor with an IC50 of 162 nM. Vanin-1 is a cell-surface-associated, glycosylphosphatidyl inositol (GPI)-anchored protein which is expressed at high levels in the kidney, liver, and small intestine[1].
Diphlorethohydroxycarmalol, a kind of phlorotannin, is an orally active α-glucosidase and α-amylase inhibitor with IC50s of 0.16 mM and 0.53 mM, respectively. Diphlorethohydroxycarmalol has anti-diabetic activities[1].
ZW290 is a compound to activate brown adipose tissue (BAT) thermogenic function. ZW290 increases the expression of uncoupling Protein 1 (UCP1) protein and inhibits ATP synthesis in BAT[1].
Phenylpropiolic acid is an endogenous metabolite.