IGF-I (24-41) is amino acids 24 to 41 fragment of Insulin-like Growth Factor I (IGF-I). IGF-I is partly responsible for systemic GH activities although it possesses a wide number of own properties (anabolic, antioxidant, anti-inflammatory and cytoprotective actions)[1].
Setogepram (PBI-4050) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84[1]. Setogepram (PBI-4050) decreases renal, liver and pancreatic fibrosis[1][2]. Setogepram (PBI-4050) exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions[2].
Cholecystokinin Octapeptide, desulfated is a synthetic desulfated octapeptides of cholecystokinin (CCK)[1].
Leriglitazone (Hydroxypioglitazone) hydrochloride, a metabolite of pioglitazone. Leriglitazone (Hydroxypioglitazone) hydrochloride PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone (Hydroxypioglitazone) hydrochloride binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM，Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50 of 680 nM[1].
NVP-DPP728 dihydrochloride is a potent, selective and orally active dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 11 nM. NVP-DPP728 dihydrochloride can be used for the research of diabetes mellitus[1][2].
Isopropamide iodide is a long-acting quaternary anticholinergic agent. Isopropamide iodide is used in peptic ulcer and other gastrointestinal disorders marked by hyperacidity and hypermotility[1][2].
Hexadecanal (Palmitaldehyde) is a free fatty aldehyde present in animals[1].
BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 52 nM.
L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
Diadenosine pentaphosphate pentalithium is an endogenous vasoactive purine dinucleotide which has been isolated from thrombocytes. Diadenosine polyphosphates (ApnA, n=2–7) have been identified as constituents of secretory vesicles such as in platelets, chromaffin cells, Torpedo synaptic terminals and brain synaptosomes[1][2].
Amitriptyline is a common oral anticholinergic. Amitriptylinehas anticholinergic properties. Amitriptyline can be used to quantifyanticholinergic adverse reactions in patients taking amitriptyline and placebo[1].
Lacto-N-fucopentaose II (LNFP II) is a sialyl-Lewis, hapten of human Lewis bloodgroup determinant. Lacto-N-fucopentaose II monosialo-ganglioside/glycolipid and sialyl derivative, CA 19-9, is a molecular tumour markers (TM) for biliopancreatic malignancy[1].
Vitamin D3-D7 (Cholecalciferol-D7) is the deuterium labeled Vitamin D3. Vitamin D3 (Cholecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells[1][2].
Omeprazole(Prilosec) is a proton pump inhibitor used in the treatment of dyspepsia.Target: Proton PumpOmeprazole is a proton pump inhibitor used in the treatment of dyspepsia, peptic ulcer disease, gastroesophageal reflux disease, laryngopharyngeal reflux, and Zollinger-Ellison syndrome. Omeprazole virtually eliminated intragastric acidity in all patients: the median 24 hour intragastric pH rose from 1.4 to 5.3 and the mean hourly hydrogen ion activity fell from 38.50 to 1.95 mmol(mEq)/1 (p less than 0.001). This inhibition of 24 hour intragastric acidity is more profound than that previously reported with either cimetidine 1 g daily or ranitidine 300 mg daily [1]. The pharmacokinetics of omeprazole were studied in a group of healthy male subjects after single and repeated oral doses of 30 and 60 mg. Absorption of omeprazole from its enteric-coated formulation was unpredictable. There was a highly significant increase in the area under the plasma concentration time curve (AUC) after repeated dosing. Omeprazole increases its own relative availability following repeated dosing. This may be due to inhibition of gastric acid secretion by omeprazole which is an acid-labile compound [2].Clinical indications: Duodenal ulcer; Endocrine tumor; Esophagitis; Gastroesophageal reflux; Helicobacter pylori infection; Stomach ulcer; Zollinger-Ellison syndromeToxicity: Symptoms of overdose include confusion, drowsiness, blurred vision, tachycardia, nausea, diaphoresis, flushing, headache, and dry mouth.
Isomalt (Palatinitol), a well-tolerated, non-toxic polyol and a protein-stabilizing excipient, stabilizes lactate dehydrogenase (LDH) moderately during freeze-drying, and performs better during storage. Isomalt is traditionally used as a sweetening agent in the food industry and as a tabletting excipient for pharmaceutical purposes[1].
Formic acid-d5 (ammonium salt) is the deuterium labeled Formic acid ammonium salt[1]. Formic acid ammonium salt is an endogenous metabolite.
3-Methyl-L-histidine is a biomarker for meat consumption, especially chicken. It is also a biomarker for the consumption of soy products.
CD31 (PECAM-1) is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation[1]-[5].
Ferroptosis-IN-4 (compound 6k) is a ferroptosis inhibitor with EC50 value of 20 μM. Ferroptosis-IN-4 has no obvious cytotoxicity. Ferroptosis-IN-4 has a protective effect in glycerol-induced RM-AKI mice with alleviating kidney dysfunction[1].
3α-Akebonoic acid is a α-glucosidase inhibitor with an IC50 value of 0.035 mM. 3α-Akebonoic acid shows antibacterial activity and cytotoxicity[1].
H-Trp-Glu-OH is a selective, reversible and cell-permeable PPARγ with a Kd of ~8 µM. H-Trp-Glu-OH might be developed as a possible lead compound in diabetes research[1].
BM 15766 sulfate is an inhibitor of 7-dehydrocholesterol δ7-reductase and reduces plasma cholesterol levels. BM 15766 sulfate is a hypolipidemic agent[1][2].
BAY-588 is a selective inhibitor of GLUT1 with an IC50 value of 1.18μM[1].
Benzylacetone is an aromatic compound from agarwood[1]. Benzylacetone exhibits potent and reversible antityrosinase (mushroom) activity， with IC50s of 2.8 mM and 0.6 mM for monophenolase and diphenolase, respectively[2]. Benzylacetone has appetite-enhancing and locomotor-reducing effects[3].
MK-0941 is a potent, orally active and allosteric glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 has potential in the treatment of type 2 diabetes[1].
GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM)[1][2].
Sebetralstat is a plasma kallikrein inhibitor (WO2016083820). Sebetralstat can be used for the research of metabolic diseases[1].
Anti-NASH agent 1 (compound 3d)，a derivative of Elafibranor (HY-16737)，is a potent agonist of PPAR-α/δ，targeting to nonalcoholic steatohepatitis (NASH). Anti-NASH agent 1 (3-10 mg/kg; 4 weeks) improves hyperlipidemia，liver fat degeneration and liver inflammation in Methionine-choline deficiency (MCD) induced NASH mice model. Anti-NASH agent 1 shows low liver toxicity and potent liver protection effect[1].
MSDC-0602, a PPARγ-sparing thiazolidinedione (TZD), interacts with the mitochondrial pyruvate carrier (MPC) and inhibits its activity and are effective for treatment of type 2 diabetes with reducing risk of PPARγ-mediated side effects[1][2].
GNF2133 is a selective DYRK1A inhibitor with an IC50 value of 6 nM.