(2α,3β,4α)-2,3,19-Trihydroxyurs-12-ene-23,28-dioic acid is a saponin that can be isolated from Rubus ellipticus var. obcordatus. (2α,3β,4α)-2,3,19-Trihydroxyurs-12-ene-23,28-dioic acid inhibits α-Glucosidase with an IC50 of 1.68 mM[1].
O-Methyl Atorvastatin (hemicalcium) is an impurity of Atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, has the ability to effectively decrease blood lipids[1].
(±)-threo-3-Methylglutamic acid is a potent EAAT2/4 inhibitor. (±)-threo-3-Methylglutamic acid also is an ionotropic glutamate receptor agonist. (±)-threo-3-Methylglutamic acid inhibits glutamate uptake by rod outer segments[1][2].
Adenosine-d2 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physio
1,2,3,19-Tetrahydroxy-12-ursen-28-oic acid is a Triterpenoid that isolated from the plant of Agrimonia Pilosa with antimalarial and antidiabetic activities[1].
Q-Peptide is the angiopoietin-1 derived peptide (QHREDGS).Q-Peptide increases keratinocyte migration to improve wound healing, in diabetic mouse model. Q-Peptide accelerates wound closure[1].
Sirtuin-1 inhibitor 1 (Compound 8) is an inhibitor of Sirtuin-1 that plays important roles in obesity-induced diabetes and aging-related diseases[1].
Ac-SVVVRT-NH2 is a PGC-1α modulator that modulates the activity of the human PGC-1α promoter (114%). Ac-SVVVRT-NH2 increases PGC-1α mRNA (125%) and accumulation of intracellular lipids (128%) in subcutaneous human adipocytes. Ac-SVVVRT-NH2 can be used in the research of diseases which is modulated by PGC-1α[1].
D-Glucose-13C2-4 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
BM152054 can promote glucose utilization in peripheral tissues by enhancing insulin action.
4,5-Dimethoxybenzene-1,2-diamine 4,5-Dimethoxybenzene-1,2-diamine can be used as a standard for the determination of methyldiacetaldehyde, an intermediate product of glycolysis and a diabetic ketone Biomarkers of acidosis[1].
Neopuerarin B is an isoflavones isolated from the water extraction of the dried roots of Pueraria lobata (Willd.). Neopuerarin B shows significant hepatoprotective effect[1].
2-Methylsuccinic acid is a normal metabolite in human fluids and the main biochemical measurable features in ethylmalonic encephalopathy.
Phenformin (1-phenethylbiguanide) is an orally active antidiabetic and anticancer agent. Phenformin has an incidence of associated lactic acidosis. Phenformin acts through acting AMPK activation and blocking mTOR pathway. Phenformin is also a substrate of P-glycoprotein (P-gp), and an OXPHOS inhibitor. Phenformin induces cancer cell apoptosis[1][2].
D-Glucose-13C,d is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical sign
Phloretin(NSC 407292; RJC 02792) is a dihydrochalcone, a type of natural phenols. Phloretin inhibits the active transport of glucose into cells by SGLT1 and SGLT2.IC50 Value: 49 +/- 12 microM [4]Target: SGLT1/2in vitro: Phlorizin blocks glucose transport across the renal tubule at concentrations in renal blood and tissue in the range of 10-5 to 10-7 M [1]. PT significantly enhanced glycerol release and inhibited the adipogenesis-related transcription factors. PT also promoted phosphorylation of AMP-activated protein kinase and increased activity of adipose triglyceride lipase and hormone-sensitive lipase in 3T3-L1 cells [2]. Phloretin induced obvious cytotoxicity against BEL-7402 cells with IC50 of 89.23 microg/mL. The growth curve demonstrated decreased growth of the cells as phloretin concentration increased [3]. D-glucose-transport activity was observed with a Km for D-glucose of 3.4 +/- 0.2 mM (mean +/- S.E.M.) and was inhibited by cytochalasin B (IC50= 0.44 +/- 0.03 microM), HgCl2 (IC50)= 3.5 +/- 0.5 microM), phloretin (IC50= 49 +/- 12 microM) and phloridzin (IC50= 355 +/- 67 microM) [4].in vivo: The effect of phloridzin orally doses 5, 10, 20 and 40 mg/kg body weight on diabetes was tested in a streptozotocin-induced rat model of diabetes type 1. From beneficial effect of this compound is significant reduction of blood glucose levels and improve dyslipidemia in diabetic rats [5].
D-myo-Inositol-1,4,5-triphosphate sodium salt is the hexapotassium salt of D-myo-Inositol 1,4,5-trisphosphate (1,4,5-IP3), which is a second messenger that stimulates the discharge of calcium from the endoplasmic reticulum.
Efaroxan hydrochloride is a potent and selective α2-adrenoceptor antagonist, antidiabetic activity. Efaroxan hydrochloride is a selective I1-Imidazoline receptor antagonist and can be used for the research of cardiovascular disease[1][2][3].
Ro 23-7637 is an orally active, efficacious antiobesity agent[1].
LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively[1]. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively[2]. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy[3].
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].
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].
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].
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.
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].
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].
Arginase is an enzyme of the urea cycle. Arginase catalyzes the hydrolysis of L-arginine to L-ornithine and urea[1].
GSK3987 is a pan LXRα/β agonist with EC50s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation[1].
MK8722 is a potent and systemic pan-AMPK activator.
Betazole (Ametazole), a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity[1][2][3].