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].
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].
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].
ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation[1].
LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM[1][2].
Methyl anisate is an endogenous metabolite.
(R)-Vitamin D2 is the inactive isomer of Vitamin D2 (HY-76542), and can be used as an experimental control. Vitamin D2 (Ergocalciferol), drived from plant sources or dietary supplements, could be used as supplement of Vitamin D[1][2].
Insulin alpha-chain (1-13) is a human leucocyte antigen (HLA)-DR4-restricted epitope comprising the first 13 amino acids of the insulin A-chain[1].
Peptide YY (PYY) is a gut hormone that regulates appetite and inhibits pancreatic secretion. Peptide YY (PYY) can mediate its effects through the Neuropeptide Y receptors.
Stearic acid-d5 is the deuterium labeled Stearic acid. Stearic acid is a long chain dietary saturated fatty acid which exists in many animal and vegetable fats and oils.
Hydrocortisone hemisuccinate (Hydrocortisone 21-hemisuccinate), a physiological glucocorticoid, and is an orally active steroidal anti-inflammatory drug (SAID). Hydrocortisone hemisuccinate inhibits proinflammatory cytokine activity, with IC50s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone hemisuccinate can be used for the research of ulcerative colitis (UC)[1][2][3].
α-Glycosidase-IN-1 (compound MZ7) is a potent α-GLY (α-Glycosidase) inhibitor, with an IC50 of 44.72 nM and a KI of 41.74 nM. α-Glycosidase-IN-1 also shows inhibition profile against human carbonic anhydrase isoenzymes I and II (hCA I and hCA II), and acetylcholinesterase (AChE), with IC50 values of 104.87, 100.04, and 654.87 nM, respectively. α-Glycosidase-IN-1 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy[1].
Bethanechol Chloride is a selective muscarinic receptor agonist without any effect on nicotinic receptors.Target: mAChRBethanechol is a parasympathomimetic choline carbamate that selectively stimulates muscarinic receptors without any effect on nicotinic receptors. Unlike acetylcholine, bethanechol is not hydrolyzed by cholinesterase and will therefore have a long duration of action. Oral bethanechol significantly improves contraction pressures and bolus transit in the smooth muscle portion of the esophagus in patients with severe IEM [1]. Bethanechol has potential benefit in the treatment of cerebral palsy [2].
NNMTi is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50=1.2 μM) and selectively binds to the NNMT substrate-binding site residues[1]. NNMTi promotes myoblast differentiation in vitro and enhances fusion and regenerative capacity of muscle stem cells (muSCs) in aged mice[2].
Lucidal (Lucialdehyde C) is a natural lanostante-type triterpene aldehyde that shows inhibitory effects against α-glucosidase (Glucosidase) with an IC50 of 0.635 mM. Lucidal has anticancer and antidiabetic effects[1][2].
MIF-IN-6 (compound 2d) is a potent macrophage migration inhibitory factor (MIF) inhibitor with an IC50 of 1.4 μM and a Ki value of 0.96 μM, respectively. MIF-IN-6 attenuates MIF-induced ERK phosphorylation and inhibits proliferation of A549 cells[1].
FXR agonist 5 (compound 1) is a FXR agonist. FXR agonist 5 can be used for research in diseases or disorders caused by metabolic inflammation[1].
Evogliptin tartrate is a potent, orally bioavailable and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, with antidiabetic activity. Evogliptin tartrate has potential for anti-atherosclerosis therapy that targets arterial inflammation[1].
PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC50 value of 6.4 µM. PCSK9-IN-10 increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 reduces atherosclerosis progression. PCSK9-IN-10 has the potential for the research of hyperlipidemia[1].
WM-662 is a WDR5-MYC interaction inhibitor, with an IC50 of 18 μM. WM-662 has potential for the research of cancer, aging, and neurodegenerative disorders[1].
Pegbelfermin (BMS-986036) is a polyethylene glycol-modified (PEGylated) analogue of human fibroblast growth factor 21 (FGF21). Pegbelfermin can be used for the research of nonalcoholic steatohepatitis (NASH)[1][2].
Glibornuride is a blocker of ATP-sensitive K+ channels (KATP channel) with a pKi of 5.75[1]. Antidiabetic agent[2].
VIP (1-12), human, porcine, rat, ovine is a vasoactive intestinal peptide (VIP) fragment. VIP (1-12), human, porcine, rat, ovine is a ligand for the CD4 (T4)/human immunodeficiency virus receptor[1][2].
cis-Ferulic acid 4-O-β-D-glucopyranoside (compound 7) is a phenolic glycosid, which can be isolated from Nitraria sibirica.. cis-Ferulic acid 4-O-β-D-glucopyranoside exhibits antioxidant activity and potent inhibitory effect on Phosphatase PTP1B[1].
Monoethylglycinexylidide is a metabolite of Lidocain (HY-B0185) via oxidative N-deethylation of Lignocaine by liver cytochrome P-450 enzymes in the liver[1].
Human PTH-(1-31) amide is a PTH analog. Human PTH-(1-31) amide stimulate phosphatidylcholine hydrolysis and stimulates adenylyl cyclase release[1].
4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic[1][2].
Novokinin TFA is a peptide agonist of the angiotensin AT2 receptor[1].
Acetylvaline is an endogenous metabolite.