Acetic acid-d3 is a the deuterium labeled Acetic acid (HY-Y0319) [1].
Azosemide, a sulfonamide loop diuretic, is a potent NKCC1 inhibitor with IC50s of 0.246 µM and 0.197 µM for hNKCC1A and NKCC1B, respectively[1].
GIP (1-39) (Gastric inhibitory peptide (1-39) (porcine)) is an insulinotropic peptide that stimulats insulin secretion from rat pancreatic islets. GIP (1-39) at 100 nM was able to significantly increase intracellular Ca2+ concentration ([Ca2+]i), and capable of enhancing exocytosis[1].
Allitol is a rare natural polyol that can be used as a sweetener. Allitol is an important intermediate for the preparation of the agents which against diabetes, cancer, and viral infections, including AIDS[1].
GRA Ex-25 is an inhibitor of glucagon receptor, with IC50 of 56 and 55 nM for rat and human glucagon receptors, respectively.
LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR[1].
Elafibranor is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively.
LY 295427 is a LDL receptor modulator and a hypocholesterolemic agent. LY 295427 derepresses the transcription of the LDLR (LDL Receptor). LY 295427 can be used for hypercholesterolemia research[1][2][3].
KW-8232, an orally active anti-osteoporotic agent, and can reduces the biosynthesis of PGE2[1].
h-NTPDase8-IN-1 (compound 2d) is a sulfamoyl-benzamides based and selective inhibitor for h-NTPDases8 (IC50=0.28 μM). h-NTPDases8 is involved in a variety of physiological and pathological functions，such as thrombosis，diabetes，inflammation，and cancer[1].
Camellianin B, a flavonoid compound, is a Camellianin A metabolite. Camellianin B has antioxidant and angiotensin converting enzyme (ACE) inhibitory activities[1][2].
Saxagliptin H2O(BMS477118 H2O) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.IC50 value: 26 nM [1]Target: DPP4in vitro: Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9) [2]. Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion.in vivo: Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT [4].
Orotic acid-13C,15N2 (monohydrate) is the 13C and 15N labeled Orotic acid[1]. Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats[2][3][4].
Glyurallin A (Compound 79) is isolated from the naturalGlycyrrhiza uralensis. Glyurallin A inhibitsα-Glucosidase(HY-P2802)(IC50=0.3 μM). Glyurallin A can be used in the study of anti-diabetes[1].
Thioquinapiperifil (KF31327 free base), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC50 of 0.074 nM) inhibitor, is used for sexual enhancement study[1][2].
Setmelanotide acetate (RM-493 acetate) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively[1].
NCGC00188636 is a novel covalent pyruvate kinase (PYK) inhibitor. NCGC00188636 blocks nucleotide binding to the active site of pyruvate kinase. NCGC00188636 can be used for the research of the metabolism of many organisms and cell types.
Valibose An α-glucosidase inhibitor. Valibose ameliorated metabolic disturbance of glucose and lipids. valibose markedly reduced level of serum BUN and NAG, and decreased the weight index of kidney.
DIPQUO is an activator of the bone marker alkaline phosphatase (ALP), with an EC50 of 6.27 μM in C2C12 cells. DIPQUO promotes mouse and human osteoblast differentiation via activation of p38 MAPK-β[1].
2-Tetradecylthio acetic acid is a pan-peroxisome proliferator activated receptor (pan-PPAR) activator. 2-Tetradecylthio acetic acid induces hypolipidemia. 2-Tetradecylthio acetic acid reduces plasma lipids and enhances hepatic fatty acid oxidation in rodents. 2-Tetradecylthio acetic acid increases the expression of genes involved in fatty acid uptake, activation, accumulation, and oxidation[1][2].
Asfotase alfa (ENB-0040) is a bone-targeted genetically engineered glycoprotein. Asfotase alfa increases the survival rate, bone mineralization and bone length and prevents mineralization defects of the feet, rib cage, lower limbs, jaw bones in Akp2−/− knockout mice. Asfotase alfa can be used for the research of perinatal, infantile, and juvenile-onset hypophosphatasia (HPP)[1].
1-Isomangostin is an inhibitor of pancreatic lipase. 1-Isomangostin inhibits porcine pancreatic lipase with an IC50 of 34.5 μM. 1-Isomangostin has anti-obesity activity[1].
Maxacalcitol (22-Oxacalcitriol) is non-calcemic vitamin D3 analog and ligand of VDR-like receptors. IC50 value:Target: Maxacalcitol (22-Oxacalcitriol)suppresses parathyroid hormone (PTH) mRNA expression in vitro and in vivo. Maxacalcitol exhibits similar effects to calcitriol in osteoblast-like cells. Maxacalcitol(22-Oxacalcitriol) inhibits tumor growth of osteosarcoma in vitro in combination with all-trans retinoic acid.
LH-21 is a potent in vivo neutral cannabinoid CB1 receptor antagonist. LH-21 reduces food intake and body weight gain in obese Zucker rats., and displays efficacy as a feeding inhibitor[1].
D-Glucose-6-phosphate disodium salt is a glucose sugar phosphorylated at the hydroxy group on carbon 6[1].
Sibutramine hydrochloride monohydrate is a novel 5-HT (serotonin) and noradrenaline reuptake inhibitor (SNRI). The IC50 for Sibutramine block of voltage-gated K+ channel (KV)4.3 is 17.3 μM.
GPi688 is a potent and orally active glycogen phosphorylase (GPa) inhibitor with IC50s of 19 nM, 61 nM and 12 nM for human liver GPa, rat liver GPa and human skeletal muscle GPa, respectively[1]. GPi688 can inhibit glucagons-mediated glucose output in rat primary hepatocytes. GPi688 can be used for researching glucagon-mediated hyperglycaemia[2].
MF-438 is a potent and orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor with an EC50 of 2.3 nM for rSCD1[1].
CAY10746 is a selective Rho kinase (ROCK) inhibitor. CAY10746 has inhibitory activity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR)[1].
Methylophiopogonone B, a homoisoflavonoidal compound that could be isolated from Ophiopogonis Tiber, could scavenge •OH and H2O2 in vitro to a certain extent[1][2].