21 products were found matching "Cay10628-100"!

3,3',5-Triiodo-L-thyronine (T3) is a thyroid hormone. It is produced by 5'-monodeiodination of the prohormone thyroxine (T4) in various tissues, including liver and kidney. T3 is an agonist of thyroid hormone receptors TRalpha and TRbeta (Kis = 2.3 nM for both) that modulates diverse biological properties, including...

Paraxanthine is an active metabolite of caffeine (Cay-14118). It is formed via N3-demethylation of caffeine by the cytochrome P450 (CYP) isoform CYP1A2. Paraxanthine is an adenosine A1 and A2 receptor antagonist (Kis = 35 and 22 µM, respectively). In vivo, paraxanthine (30 mg/kg) increases striatal cGMP and...

Dimetridazole is a nitroimidazole-based compound with antibacterial and anticoccidial activity. It was once widely used in the treatment of parasitic infections in poultry, cattle, swine and farmed fish until suspected to be carcinogenic and mutagenic to humans. Hydroxy dimetridazole is a metabolite of dimetridazole...

Many of the products generated by alkylating agents on DNA can be efficiently repaired by normal base excision repair (BER). Some poly(ADP-ribose) polymerases (PARPs) assist in the repair of single-strand DNA nicks, an important step in BER. Olaparib is a potent inhibitor of PARP1 and PARP2 (IC50 = 5 and 1 nM,...

GS-9620 is an orally available agonist of toll-like receptor 7 (TLR7, EC50 = 291 nM) with 30-fold selectivity over TLR8 (EC50 = 9 µM). It has been shown to stimulate a TLR7 immune response in two different animal models of chronic hepatitis B infection and to inhibit HIV-1 infection in human peripheral blood...

Carazolol is a beta-adrenergic receptor (beta-AR) ligand (Kds = 0.2, 0.03, and 4.47 nM for the human beta1-, beta2-, and beta3-ARs, respectively). It reduces epinephrine-induced increases in mean arterial blood pressure and heart rate in conscious pigs when administered at a dose of 10 µg/kg. Carazolol has been...

The human-Embryonic ectoderm development (EED) protein is a WD40 repeat-containing protein that forms part of the Polycomb repressive complex 2 (PRC2). The PRC2 core complex contains the catalytic subunit EZH2 (Enhancer of zeste 2), SUZ12 (Suppressor of zeste) and EED. The EED subunit does not contain...

JWH 098 (Cay-10680) is a potent synthetic cannabinoid (CB), activating the CB1 receptor with a Ki value of 4.5 nM and the CB2 receptor with a Ki value of 1.88 nM. Its effects in cells and animals are unknown. This product is intended for research and forensic applications.Formal Name:...

16,16-dimethyl PGA2 is a metabolism-resistant analog of PGA2 with a prolonged in vivo half-life. It inhibits the proliferation of Sendai virus in cultured African green monkey kidney cells by >90% at a concentration of 4 µg/ml. Daily infusion of 10 µg of 16,16-dimethyl PGA2 methyl ester into mice infected with...

Gamma-aminobutyric acid (GABA) is the primary inhibitory neurotransmitter in the central nervous system, causing a hyperpolarization of the membrane through the opening of a Cl- channel associated with the GABAA receptor (GABAA-R) subtype. GABAA-Rs are important therapeutic targets for a range of sedative,...

Leukotriene A4 (LTA4) hydrolase/aminopeptidase is a bifunctional zinc metalloenzyme that both catalyzes the synthesis of LTB4 (Cay-20110) from LTA4 and cleaves the chemotactic peptide Pro-Gly-Pro. SC-57461A is a potent, orally active inhibitor of LTA4 hydrolase that blocks ionophore-stimulated LTB4 synthesis in...

The ion channels activated by glutamate are typically divided into two classes. Glutamate receptors that are activated by kainate and alpha-amino-3-hydroxy-5-methyl-4-isoxalone propionic acid (AMPA) are known as kainate/AMPA receptors (K/AMPAR). Those that are sensitive to N-methyl-Daspartate (NMDA) are designated...