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].
(3R)-7-hydroxy-3-(4-hydroxybenzyl)chromane is a homoisoflavonoid. (3R)-7-hydroxy-3-(4-hydroxybenzyl)chromane increases the level of alkaline phosphatase (ALP) activity. (3R)-7-hydroxy-3-(4-hydroxybenzyl)chromane promotes mesenchymal stem cells (MSCs) osteogenesis, but cannot enhance MSCs proliferation. (3R)-7-hydroxy-3-(4-hydroxybenzyl)chromane can be used for osteoporosis research[1].
(-)-Fucose is classified as a member of the hexoses, plays a role in A and B blood group antigen substructure determination, selectin-mediated leukocyte-endothelial adhesion, and host-microbe interactions.
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.
Pparδ agonist 8 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) is a member of the intranuclear receptor transcription factor superfamily that plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Pparδ agonist 8 has the potential for the research of non-alcoholic fatty liver disease (NAFLD) (extracted from patent WO2021169769A1, compound TM2)[1].
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].
Carbazeran, a potent phosphodiesterase inhibitor, is aldehyde oxidase substrate. Carbazeran can be used for the research of metabolic disease[1].
Decanoyl-L-carnitine chloride is an ester derivative of L-carnitine, which is an important cofactor of fatty acid metabolism[1].
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].
Sp-cAMPS triethylamine, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS triethylamine is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS triethylamine binds the PDE10 GAF domain with an EC50 of 40 μM[1][2][3].
BAY-588 is a selective inhibitor of GLUT1 with an IC50 value of 1.18μM[1].
SDZ-62-434 is a platelet-activating factor (PAF) antagonist. SDZ-62-434 has antiproliferative activity in human solid and haematological malignancies[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].
GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner.IC50 value: 7.32 (pEC50) [1]Target: GPR40GW9508 is shown to be at least 100-fold selective against 220 other GPCRs, 60 kinases, 63 proteases, seven integrins and 20 nuclear receptors including PPARα, δ and γ (pEC50 4.0, 4 and 4.9, respectively). GW9508 produces a concentration-dependent increase in intracellular Ca2+ concentrations via GPR40 receptor activation and the GPR120 receptor. GW9508 is active as an agonist at both GPR40 and GPR120, it is approximately 100-fold selective for GPR40 with respect to GPR120. GW9508 produces a concentration-dependent increase (pEC50=6.14) in glucose-stimulated insulin secretion at high glucose levels (25 mM). GW9508 dose dependently stimulated insulin secretion in a glucose-sensitive manner in MIN6 cells. Furthermore, GW9508 is able to potentiate the KCl-mediated increase in insulin secretion in MIN6 cells. [1] GW9508 induced hyperpolarization and opening of KATP channels in rat β-cells. [2] GW9508 inhibits CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. GW9508 further suppresses expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-α and IFN-γ. GW9508 also inhibits CCL5 and CXCL10 production by normal human epidermal keratinocytes. [3]
Vasopressin V2 receptor antagonist 1 (Compound 4g) is a vasopressin V2 receptor (V2R) antagonist with a Ki of 3.8 nM. Vasopressin V2 receptor antagonist 1 can be used for autosomal dominant polycystic kidney disease (ADPKD) research[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].
EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively[1].
Sebetralstat is a plasma kallikrein inhibitor (WO2016083820). Sebetralstat can be used for the research of metabolic diseases[1].
Exendin (9-39) is a specific and competitive glucagon-like peptide-1 receptor antagonist.
VU661, a phenazine carboxamide, is a modulator of circadian rhythms to produce a period lengthening of the circadian rhythm. VU661 is a redox-active small molecule [1].
ALDH2 modulator 1 is a potent and orally active aldehyde dehydrogenase-2 (ALDH2) modulator. ALDH2 modulator 1 reduces blood alcohol levels in mice[1].