15 products were found matching "Cay17355"!

Saclofen is a sulfonic analog of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) that acts as a competitive antagonist of the GABAB receptor (IC50 = 7.8 µM). This compound can be used to determine the functional roles for the GABAB receptor as a mediator of slow inhibitory postsynaptic potentials in...

Atazanavir is an azapeptide inhibitor of HIV-1 protease (Ki = 2.66 nM). It has antiviral activity against a variety of HIV-1 strains in several cell types with EC50 values ranging from 2.62 to 5.28 nM. Atazanavir exhibits a minor synergistic effect when used in combination with the reverse transcriptase inhibitor...

UR-144 (Cay-11502) is a potent synthetic cannabinoid (CB) which preferentially binds the peripheral CB2 receptor (Ki = 1.8 nM) over the central CB1 receptor (Ki = 150 nM). UR-144 N-pentanoic acid metabolite is an expected phase I metabolite of UR-144, based on the metabolism of similar cannabimimetics. This...

Glucose transporter 1 (Glut1) is an inducible carrier of pentoses and hexoses, including glucose. STF-31 is an inhibitor of Glut1 (IC50 = ~1 µM) that blocks glucose uptake. It induces necrosis in cancer cells that lack the von Hippel-Lindau tumor suppressor gene, which overexpress Glut1. Although STF-31 binds Glut1,...

Temoporfin is a synthetic chlorin with light-activated actions. When administered systemically, temoporfin accumulates in tumor cells. When stimulated with light (650-652 nm) in the presence of oxygen, reactive oxygen species are generated, leading to necrosis within the tumor. Different approaches to using...

Quinacrine analog 34 is an inhibitor of autophagy with a minimum effective concentration (MEC) of 0.5 µM in U2OS cells. It induces lysosomal deacidification and accumulation of LC3-II in the same cells when used at concentrations of 0.5 or 3 µM.Formal Name:...

AB-PINACA (Cay-14038) is a synthetic cannabinoid identified in illegal herbal products. Variations of AB-PINACA have been synthesized including derivatives that include a fluorine atom added to the terminal carbon of the pentyl group. 5-fluoro AEB is an analog of AB-PINACA characterized by the replacement of the...

The free fatty acid receptor 1 (FFAR1, GPR40) is highly expressed in pancreatic beta-cells and activated by medium and long-chain fatty acids. There is evidence of a link between FFAR1 (GPR40) and the ability of fatty acids to amplify glucose-stimulated insulin secretion, making this signaling pathway a potential...

Reparixin is an allosteric antagonist of chemokine (C-X-C motif) receptor 1 (CXCR1) and CXCR2 (IC50s = 1 and 100 nM, respectively). In vivo, reparixin (3, 15, and 30 mg/kg) reduces ischemia and reperfusion-induced hepatic polymorphonuclear leukocyte (PMN) recruitment, hepatic myeloperoxidase (MPO) levels, and serum...

Trimethylamine N-oxide (TMAO) is a metabolite of choline, phosphatidylcholine, and L-carnitine (Cay-21489). It is formed by gut microbiota-mediated metabolism of choline, phosphatidylcholine, and L-carnitine to TMA followed by oxidation of TMA by flavin-containing monooxygenase 3 (FMO3) in the liver. Dietary...

The alpha1-adrenergic receptors are Gq protein-coupled receptors that play a key role in the modulation of sympathetic nervous system activity and are the site of action for therapeutic agents, such as antihypertensive drugs. A-61603 is a selective alpha1A-adrenergic receptor agonist that is at least 35-fold more...

Temafloxacin is a fluoroquinolone antibiotic that acts as a DNA topoisomerase inhibitor. It has broad antimicrobial activity against gram-positive and gram-negative bacteria, such as S. pneumoniae, M. hominis, and anaerobic bacteria, including B. fragilis.Formal Name:...