15 products were found matching "Cay70210"!

CAY10404 is an inhibitor of COX-2 (IC50 = 50 = >500 µM). CAY10404 inhibits the proliferation of SH-EP and SH-SY5Y neuroblastoma cells (IC50s = ~60 µM for both), and induces apoptosis and cell cycle arrest at the G2/M phase in the same cells. It inhibits carrageenan-induced paw edema in rats when administered at a...

DPP (IV) inhibitors have emerged as a new class of oral antidiabetic agents. These inhibitors promote glucose homeostasis by inhibiting degradation of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) by DPP (IV). GLP-1 extends the action of insulin while suppressing the release...

Cayman's GGT Activity Assay Kit provides a convenient method of detecting GGT activity in plasma, serum, and tissue lysates. In this assay, GGT catalyzes the transfer of the gamma-glutamyl group from L-gamma-glutamyl-p-nitroaniline (gammaGpNA) to glycylglycine resulting in the liberation of the colored product...

Cayman's TXAS Inhibitor Screening Assay Kit provides a robust and easy-to-use platform for identifying novel inhibitors of human TXAS. The assay uses a TAMRA-conjugated TXAS-specific probe suitable for fluorescence polarization (FP)-based screening of TXAS inhibitors. Inhibitors of TXAS displace the fluorescent...

5-Aminosalicylic acid (5-ASA) is a non-steroidal anti-inflammatory drug (NSAID) and an active metabolite of sulfasalazine (Cay-15025), balsalazide (Cay-18680), and olsalazine (Cay-23661). It is formed from these prodrugs by bacterial azoreductases in the intestinal lumen. 5-ASA selectively inhibits COX-2 over COX-1...

LY83583 is an inhibitor of soluble guanylate cyclase and of cGMP production. It inhibits soluble guanylate cyclase in human platelets with an IC50 value of 2 µM. LY83583 also inhibits leukotriene synthesis in guinea pig lung and rat peritoneal cells with an IC50 value of 1.8 µM and is a noncompetitive inhibitor of...

IMMA is a cannabinoid (CB) receptor 2 inverse agonist (Ki = 435 nM for recombinant human CB2). It is selective for CB2 over CB1 receptors (Ki = >20 µM). IMMA (0.001-1 µM) reduces basal production of inositol phosphate and increases forskolin-induced accumulation of cAMP in HEK293 cells expressing human CB2...

Indomethacin is a potent but non-selective inhibitor of both COX-1 and COX-2 in sheep and humans. Structurally, indomethacin is a substituted indole acetic acid, wherein the carboxylate can be derivatized as an ester or amide. These derivatives show enhanced selectivity for the COX-2 isoform. For example, the IC50...

Indomethacin is a potent but non-selective inhibitor of both COX-1 and COX-2 in sheep and humans. Structurally, indomethacin is a substituted indole acetic acid, wherein the carboxylate can be derivitized as an ester or amide. These derivatives show enhanced selectivity for the COX-2 isoform. For example, the IC50...

O-Acetyl Salicylhydroxamic Acid (O-ASHA) is an irreversible, non-selective inhibitor of COX-1 and COX-2. Aspirin is the best-studied example of an irreversible COX inhibitor, acting via the acetylation of the active site serine residue 529 in human COX-1. O-ASHA inhibits ovine COX-1 in a time-dependent, irreversible...

N-(2-phenylethyl)-indomethacin amide (N-2PIA) is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2. N-2PIA inhibits human recombinant and ovine COX-2 with IC50 values of 0.06 and 0.125 µM, respectively. It is over 400 times less potent as an inhibitor...

N-(3-pyridyl)-indomethacin amide (N-3PyIA) is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2. N-3PyIA selectively inhibits human recombinant COX-2 with an IC50 of 0.052 µM. It is about 1,300 times less potent as an inhibitor of ovine recombinant...