14 products were found matching "Cay16824-%25"!

tetranor-PGFM is the major urinary metabolite of PGF2alpha. Normal healthy females excrete 7-13 µg of tetranor-PGFM per day compared to 11-59 µg/24 hours for healthy males. In pregnant females, tetranor-PGFM levels in the urine are 2 to 5-fold higher and diminish to pre-pregnancy levels soon after labor.Formal Name:...

The serine hydrolase known as alpha/beta-hydrolase domain-containing protein 6 (ABHD6) hydrolyzes 2-arachidonoyl glycerol (Cay-62160) to regulate its availability at cannabinoid receptors. WWL123 is a brain-penetrant inhibitor of ABHD6 (IC50 = 0.43 µM) that demonstrates >10-fold selectivity for ABHD6 compared to a...

Serine/arginine-rich protein kinase 1 (SRPK1) targets proteins that contain multiple serine/arginine (SR) dipeptides, including SR-rich splicing factor 1, SRSF1. SRPIN340 is an isonicotinamide compound that inhibits SRPK1 (Ki = 0.89 µM). It is about 10-fold less effective against SRPK2 and does not inhibit the...

Rifabutin is a rifamycin antibiotic. It is active against a variety of Gram-positive and Gram-negative bacteria, including 81 clinical isolates of H. pylori (MIC50 = 0.25 µg/ml), as well as S. aureus, S. pyogenes, and C. trachomatis (MICs = 0.004, 0.005, and ~0.008 µg/ml, respectively). Rifabutin (0.5 µg/ml) is also...

Acetyl-L-carnitine is an acetylated form of the essential mitochondrial metabolite L-carnitine (Cay-21489) that is catabolized by plasma esterases into carnitine. Acetyl-L-carnitine facilitates the uptake of acetyl-CoA into mitochondria during fatty acid oxidation, enhances acetylcholine production, and stimulates...

Glycopyrrolate is an antagonist of muscarinic acetylcholine receptors (mAChRs, Kis = 0.42, 1.77, 0.52, 0.78, and 1.29 nM for the M1-M5 receptors, respectively). It induces relaxation of precontracted isolated human bronchi when used at concentrations of 0.01, 0.1, or 1 µM. Glycopyrrolate reduces post-prandial...

D-Glucose is phosphorylated by glucokinase and three tissue-specific hexokinases to produce glucose-6-phosphate in humans. D-Mannoheptulose is a heptose that inhibits glucokinases and hexokinases from diverse organisms through competition with D-glucose (Ki = 0.25 mM). It blocks glucose oxidation and...

Apurinic/apyrimidinic endonuclease-1 (Ape-1) is involved in base excision repair, cleaving the phosphodiester linkage that is 5' to the abasic site to produce a single strand break. DNA base excision repair pathway inhibitor is a cell-permeable inhibitor of Ape-1 (IC50 = 3-11 µM). Although not toxic to cells by...

Promethazine is a first-generation histamine H1 receptor antagonist (Ki = 0.98 nM for the human receptor). It is selective for histamine H1 over H3 and H4 receptors (Kis = >100 and 77.6 µM, respectively, for the human receptors). Promethazine also binds muscarinic acetylcholine receptors (mAChRs, Ki = 22 nM). It...

Ezatiostat is an inhibitor of glutathione S-transferase pi 1-1 (GSTP1-1, Ki = 0.4 µM). It is selective for GSTP1-1 over GSTalpha and GSTµ family GSTs (Kis = 20-75 µM). Ezatiostat also inhibits the protein-protein interaction between GSTP1-1 and JNK1. In vivo, ezatiostat (75 mg/kg) increases the number of circulating...

Leflunomide is a synthetic isoxazol and a prodrug form of A-771726 (Cay-14404), a dihydroorotate dehydrogenase inhibitor. Leflunomide inhibits de novo pyrimidine synthesis to regulate T lymphocyte progression through the cell cycle. It inhibits proliferation and activation of T cells when used at concentrations of...

Aprepitant an antiemetic and antagonist of the neurokinin-1 (NK1) receptor (Ki = 3 nM, IC50 = 0.09 nM for the human receptor). It is selective for NK1 over NK3 receptors (Ki = 454.1 nM for human NK3). In vivo, aprepitant (1 mg/kg) prevents plasma extravasation into the esophagus of guinea pigs induced by substance P...