O-Desisobutyl-O-n-propyl Febuxostat, extracted from the patent CN 103467412, is an xanthine oxidase inhibitor[1].
L-Cysteine hydrochloride hydrate is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine hydrochloride hydrate suppresses ghrelin and reduces appetite in rodents and humans[1].
Tripeptide-32isa bioactive peptide with anti-aging effect and has been reported used as a cosmetic ingredient[1].
D-Glucose-d1-1 is the deuterium 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].
T-1095 is a selective and orally active Na+-glucose cotransporter (SGLT) inhibitor with IC50s of 22.8 µM and 2.3 µM for human SGLT1 and SGLT2, respectively. T-1095 can be used for diabetes research[1].
L-(+)-Arabinose selectively inhibits intestinal sucrase activity in a noncompetitive manner and suppresses the plasma glucose increase due to sucrose ingestion.
2'-O,4'-C-Methyleneadenosine (LNA-A) is a locked nucleic acid (LNA) and is also an adenosine analog[1].
Tripamide is an orally active sulfonamide-derived diuretic antihypertensive agent[1].
CDK8-IN-3 is an inhibitor of CDK8 extracted from patent WO2016041618A1, compound example 1.7.
N-Acetyl-D-glucosamine-13C,15N is the 13C and 15N labeled N-Acetyl-D-glucosamine. N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of gluc[1][2].
S-(2-Carboxypropyl)-L-cysteine (β-Isobuteine) is a urine metabolite, a metabolic marker of leigh-like syndrome[1].
TGR5 Receptor Agonist, a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5).IC50 value: 6.8 (pEC50, U2-OS cell assay); 7.5(pEC50, melanophore cell) [1]Target: TGR5TGR5 Receptor Agonist was profiled against more than 100 in-house and external 7TM, ion channel, enzyme, transporter, and nuclear hormone receptor selectivity assays, including FXR, another bile acid receptor, and showed significant response only in secretion of the pro-inflammatory cytokine TNFalpha (pIC50 = 6.8) in human primary monocytes following stimulation with LPS (lipopolysaccharide). In addition, TGR5 Receptor Agonist has good physicochemical properties and no measurable activity against three of the common cytochrome P450 (CYP450) isoforms (1A2, 2C9, and 2D6) or hERG dofetilide binding (pIC50 <4.3). In rat pharmacokinetic (PK) studies, however, TGR5 Receptor Agonist showed high in vivo clearance (Cl = 85 mL/min/kg) and intrinsic clearance (Clint = 48 mL/min/g) which provided a reasonable explanation for the observed poor exposure. Because the TGR5 receptor is expressed in the GI tract at levels that increase corresponding with L-cell population density, we believe that agonists such as 6 and 7 possessing poor systemic exposure are good tool compounds for directly targeting the TGR5 receptor in the GI tract via local administration (vide infra) rather than systemic exposure. Our hypothesis was that for this receptor, systemic exposure was not necessary to achieve the desired effect of stimulating GLP-1 secretion in vivo [1].
GSK3-IN-1 (compound 11) is a GSK-3 inhibitor with an IC50 value of 12 μM. GSK3-IN-1 can be used in the research of diabetes[1].
Dehydrovomifoliol is a AKT/mTOR dual inhibitor. Dehydrovomifoliol reduces lipid accumulation and lipogenesis by inhibiting the AKT/mTOR signaling pathway. Dehydrovomifoliol is used in nonalcoholic fatty liver disease research (NAFLD) .
Kushenol X, a flavonoid compound isolated from the roots of Sophora flavescens. Kushenol X is a potent β-glucuronidase and human carboxylesterase 2 (hCE2) inhibitor with IC50s of 2.07 μM and 3.05 μM, respectively[1][2].
AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM.
Picolinamide (2-Picolinamide) is an inhibitor of Poly(ADP-ribose) synthetase of nuclei from rat pancreatic islet cells[1][3].
A potent, selective, orally active inhibitor of cathepsin K with Ki of 0.1 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively; shows less or no potentcy for human cathepsin S/L/B/C (Ki=0.83/1.7/32/2500 nM); inhibits human osteoclasts bone resorption in vitro at a concentration more than 100 fold lower than that of alendronate; reduces plasma calcium level increased by PTHrP in thyroparathyroidectomized rats, decreases serum and urine C-telopeptide of type I collagen level. Osteoporosis Phase 2 Discontinued
Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research[2][3][4].
Creosol-d4 is the deuterium labeled Creosol[1]. Creosol is an endogenous metabolite.
KH-176 (KH176, Sonlicromanol) is a smal molecule ROS-redox modulator, effectively reduces increased cellular ROS levels and protects OXPHOS deficient primary cells against redox perturbation by targeting the Thioredoxin/Peroxiredoxin system; significantly improves rotarod and gait performance and reduces the degeneration of retinal ganglion cells in Ndufs4 -/- mice, shows therapeutic effects in mammalian model of Leigh Disease.
Indole-13C8,15N is the 13C and 15N labeled Indole[1]. Indole is an endogenous metabolite.
BMS-309403 is a potent, selective and cell-permeable inhibitor of fatty acid binding protein 4 (FABP4) with a Ki of less than 2 nM.
PF-07258669 is a melanocortin-4 receptor (MC4) antagonist. PF-07258669 can be used for the research of cachexia, anorexia, or anorexia nervosa[1].
Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases[1].
Leucine dehydrogenase can be purified from Bacillus spheroides. Leucine dehydrogenase catalyzed the oxidative deamination of L-leucine, L-valine, L-isoleucine, L-norvaline, L-alpha-aminobutyrate, and L-norleucine, and the reductive amination of their keto analogues[1].
Clathrin-IN-2 is potent inhibitor of clathrin mediated endocytosis (CME) with an IC50 value of 2.3 μM. Clathrin-IN-2 also has inhibitiory for dyn I GTPase with an IC50 value of 7.7 μM[1].
Bevantolol hydrochloride is a selective β1 and α1-adrenergic receptor antagonist with pKi values of 7.83, 6.9 in rat cerebral cortex, respectively. Bevantolol hydrochloride is a potent Ca2+ antagonist[1][2].
Dynasore is a cell-permeable dynamin inhibitor with an IC50 of 15 μM.
KT5720 is a cell-permeable, potent, specific, reversible, ATP-competitive inhibitor of protein kinase A (PKA), with a Ki of 60 nM[1][2].