14 products were found matching "Cay15425"!

Ticagrelor is a reversible antagonist of the platelet purinergic P2Y12 receptor (Ki = 14 nM, IC50 = 1.8 µM), which is the main receptor responsible for ADP-induced platelet aggregation. It functions by directly changing the conformation of the P2Y12 receptor to inhibit ADP binding. Formulations containing ticagrelor...

Carbamazepine is an inhibitor of sodium channels. It preferentially inhibits inactivated voltage-gated sodium channel Nav1.7 and Nav1.3 (IC50s = 406 and 900 µM, respectively) over resting (closed) Nav1.7 and Nav1.3 channels in whole-cell patch-clamp assays using HEK293 cells (IC50s = 1,584 and 2,464 µM,...

FR180204 is a potent cell-permeable inhibitor of ERK1 and ERK2 (Ki = 310 and 140 nM, respectively). It is much less effective against p38alpha (IC50 = 10 µM) and does not inhibit a range of other serine/threonine or tyrosine kinases. FR180204 blocks ERK-mediated signaling from TGF-beta to AP-1 (IC50 = 3.1 µM). It...

The generation of beta-lactamases by bacteria affords resistance to several classes of beta-lactam antibiotics, including penicillins and cephalosporins. Nitrocefin is a chromogenic cephalosporin substrate commonly used to detect beta-lactamases in bacteria. The presence of beta-lactamase activity is indicated by...

Nobiletin is a polymethoxylated flavonoid that has been found in C. unshiu and has diverse biological activities. It reduces LPS- and IFN-gamma-induced increases in inducible nitric oxide synthase (iNOS) protein levels and NO production in RAW 264.7 cells when used at concentrations of 25, 50, and 100 µM. Nobiletin...

Apixaban is an orally bioavailable, selective inhibitor of both free and prothrombinase-bound factor Xa (Kis = 0.8 nM). In vivo, apixaban has antithrombotic effects in a rabbit model of venous thrombosis. Apixaban (357.5 mg) also prevents thrombus formation without inducing adverse bleeding events in a porcine model...

Miconazole is a widely used antifungal imidazole that acts by inhibiting the 14alpha-demethylation of lanosterol, which consequently leads to the inhibition of ergosterol synthesis in fungal cell membranes. Additionally, miconazole has been shown to induce reactive oxygen species in fungal biofilms, demonstrating a...

LUF6283 is a partial agonist of GPR109A/HCA2 G protein-coupled receptors (Ki = 0.55 µM in a radioligand binding assay). It stimulates [35S]-GTPgammaS binding and increases phosphorylation of ERK in HEK293T cells expressing GPR109A/HCA2 receptors (EC50s = 3.1 and 0.32 µM, respectively). In vivo, LUF6283 (400 mg/kg...

Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI). It is phosphorylated intracellularly to its active form zidovudine-5'-triphosphate by the successive actions of thymidine kinase, thymidylate kinase, and nucleoside diphosphate kinase. Zidovudine (0.01, 0.1, and 1 µM) reduces HIV-1 p24 antigen levels...

Idebenone is a benzoquinone analog of coenzyme Q10 (Cay-11506), a natural quinone that serves as a cofactor in the electron transport chain in mitochondria. Like coenzyme Q10, idebenone is a potent lipid antioxidant that prevents the generation of free radicals. In particular, idebenone targets mitochondria,...

Lamotrigine is an anticonvulsant. It inhibits voltage-gated sodium channels (Nav) in HEK293 cells expressing recombinant human Nav1.2, Nav1.5, or Nav1.8 (IC50s = 10, 62, and 96 µM, respectively), as well as high voltage-activated calcium currents in isolated rat cortical neurons (IC50 = 12.3 µM), an effect that can...

KT182 is a potent inhibitor of alpha/beta-hydrolase domain-containing protein 6 (ABHD6) with IC50 values of 1.7, 15.1, and 0.24 nM using Neuro2a membrane proteomes, recombinant ABHD6 in HEK293T cells, and Neuro2a cells in situ, respectively. Following administration of KT182 (1 mg/kg, i.p.) in mice, ABHD6 is...