Fucoidan, a biologically active polysaccharide, is an efficient inhibitor of α-amylase and α-glucosidase. Anticoagulant, antitumor, antioxidant and antisteatotic activities[1].
Hexapeptide-3isa bioactive peptide with repair skin effect and has been reported used as a cosmetic ingredient[1].
Troxerutin, also known as vitamin P4, is a tri-hydroxyethylated derivative of natural bioflavonoid rutins which can inhibit the production of reactive oxygen species (ROS) and depress ER stress-mediated NOD activation.
Xanthine oxidoreductase-IN-4 is an orally active xanthine oxidoreductase (XOR) inhibitor. Xanthine oxidoreductase-IN-4 has inhibitory activity against XOR with an IC50 value of 29.3 nM. Xanthine oxidoreductase-IN-4 can be used for the research of hyperuricemia[1].
PPARγ-IN-2 (Compound 5a) is a PPARγ inhibitor. PPARγ-IN-2 inhibits TG accumulation in 3T3-L1 preadipocytes (EC50: 0.106 μM). PPARγ-IN-2 inhibits high-cholesterol diet (HFC)-induced obesity and related metabolic syndrome, and reduces lipid accumulation in adipose tissue[1].
Lith-O-Asp is a sialytransferase (ST) inhibitor, with IC50s of 12-37 μM.
2-Methylsuccinic acid-d6 is the deuterium labeled 2-Methylsuccinic acid[1]. 2-Methylsuccinic acid is a normal metabolite in human fluids and the main biochemical measurable features in ethylmalonic encephalopathy[2][3].
APPA is an aldose reductase inhibitor. APPA can effectively prevent apoptosis and the symptoms of Streptozotocin (HY-13753)-induced diabetes by inhibiting the polyol pathway in rats. APPA has the potential for diabetic nephropathy (DN) research[1].
N-Oleoyl glycine is a lipoamino acid, which stimulates adipogenesis associated with activation of CB1 receptor and Akt signaling pathway in 3T3-L1 adipocyte.
INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity research[1].
Efpeglenatide is a new once weekly GLP-1 Injection for Type 2 Diabetes
Canosimibe is a cholesterol absorption inhibitor extracted from patent WO2004087655A1.
GW0742 is a high affinity PPAR β/δ agonist with an IC50 of 1 nM for human PPARδ, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.
MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
Oleic acid-d2 (9-cis-Octadecenoic acid-d2) is the deuterium labeled Oleic acid. Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid[1]. Oleic acid is a Na+/K+ ATPase activator[2].
Gangliosides act as acceptors. Reaction: CMP-N-acetylneuraminate + α-N-acetylneuraminyl-(2→3)-β-D-galactosyl-R = CMP + α-N-acetylneuraminyl-(2→8)-α-N-acetylneuraminyl-(2→3)-β-D-galactosyl-R
Adenosine 5'-monophosphate disodium is an orally active purine nucleotide, and participates in ATP metabolism. Adenosine 5'-monophosphate disodium is also a ligand for adenosine 2B receptor. Adenosine 5'-monophosphate disodium can activate AMPK in skeletal muscle, and ameliorates insulin resistance and impaired glucose metabolism. Adenosine 5'-monophosphate disodium can be used for research of diabetes[1][2][3].
Adenosine-d1-1 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 phys
Trichlormethiazide sodium is an orally active thiazide diuretic, with antihypertensive effect. Trichlormethiazide sodium increases urine volume (UV), Na and K excretion and tends to improve the depressed creatinine clearance (CCRE) in acute renal failure rats model[1][2].
Ligustroflavone, extracted from Ligustrum lucidum, is a potential candidate as calcium-sensing receptor (CaSR) antagonist. Ligustroflavone exhibits protective effects against diabetic osteoporosis in mice[1].
Betazole (Ametazole) dihydrochloride, a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole dihydrochloride induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole dihydrochloride has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity[1][2][3].
DL-AP4 (2-Amino-4-phosphonobutyric acid) is a glutamate antagonist. DL-AP4 behaves as a competitive inhibitor of glutamate binding with an apparent Kd of 66 μM. DL-AP4 can be used for the research of central nervous system and visual system[1][2][3].
Kynuramine (dihydrobromide), an endogenously occurring amine, is a fluorescent substrate and probe of plasma amine oxidase[1][2].
Cochinchinenin C is a nonpolypeptide agonist of glucagon-like peptide-1 (GLP-1) receptor. Cochinchinenin C can be used for the research of diabetes[1][2].
GSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia[1][2]. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2
Pterosin A is an orally active anti-diabetic agent. Pterosin A promotes glucose uptake, increases serum insulin, and improves hyperglycemia and glucose intolerance in diabetic mice. Pterosin A can be isolated from Pteridium aquilinum[1][2].
CDK5-IN-1, a potent CDK5 inhibitor, is against CDK5 activity less than 10 nM. CDK5-IN-1 is used for kidney diseases research[1].
AST 7062601 (AST070) is a Ucp1 inducer that strongly induces endogenous Ucp1 expression in primary mouse brown adipocytes. Ucp1 refers to uncoupling protein, found in brown and beige fat cells. In mammals, UCP1 oxidizes fatty acids and uncouples ATP production in mitochondria to promote energy dissipation as heat. AST 7062601 can be used to study thermogenic, uncoupled respiration[1].
Cinnamtannin B-1 is a proanthocyanidin with multiple biological functions, including antioxidant effects. Cinnamtannin B-1 inhibits RANKL-induced osteoclastogenesis and prevents ovariectomy-induced osteoporosis in vivo[1]. Cinnamtannin B-1 can be used for the research osteoporosis and colon cancers[1][2].
(Glu13,17,20)-Osteocalcin (1-46) (mouse) is an analogue of Osteocalcin (1-46). Osteocalcin (1-46) is a osteoblast specific peptide involved in the regulation of energy metabolism[1].