8 products were found matching "Cay70710"!

LY171883 is a selective, potent, orally active antagonist of the leukotriene D4 receptor. Dissociation constants (KB) for LY171883 on guinea pig ileum and parenchyma are 0.07 and 0.34 µM, respectively. LY171883 is an inhibitor of phosphodiesterase obtained from human polymorphonuclear leukocytes (IC50 of 22.6 µM)...

The peroxisome proliferator-activated receptor gamma (PPARgamma) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones. Thiazolidinediones are a group of structurally related synthetic PPARgamma agonists with antidiabetic actions in vivo. Rosiglitazone (BRL 49653) is...

U-73122 is an inhibitor of PLC-dependent processes, however, the mechanism of action remains unclear. The IC50 values for inhibition of platelet aggregation induced by collagen or thrombin are 0.6 and 5 µM, respectively. It also exhibits inhibitory activity against HIV-1 integrase with an IC50 value of 7 µM.Formal...

Antagonists of the chemotactic and inflammatory lipoxygenase product leukotriene B4 (LTB4) have been potential drug development targets for several years. The tetrazole LY255283 is a competitive antagonist of the BLT2 receptor. It displaces radiolabeled LTB4 from guinea pig lung membrane, with an IC50 of about 100...

Wy 14643 is an agonist of peroxisome proliferator-activated receptor alpha (PPARalpha). It selectively transactivates PPARalpha over PPARgamma in a reporter assay using CV-1 mouse fibroblasts when used at a concentration of 100 µM. Wy 14643 (2 mg/kg) decreases distal colon protein levels of IFN-gamma, TNF-alpha,...

MK-571 is a cysteinyl leukotriene 1 (CysLT1) receptor antagonist (Ki = 2.1 nM in a radioligand binding assay using isolated human lung membranes). It inhibits contractions induced by leukotriene D4 (LTD4, Cay-20310) or LTE4 (Cay-20410) in histamine-primed isolated guinea pig trachea (pA2s = 9.4 and 9.1,...

BEL is a selective, potent, irreversible, mechanism-based inhibitor of myocardial cytosolic calcium-independent phospholipase A2 (iPLA2) with a Ki value of 180 nM. BEL also inhibits macrophage iPLA2 in a concentration-dependent manner with an IC50 value of 60 nM and is an effective enzyme-activated irreversible...

The peroxisome proliferator-activated receptor-gamma (PPARgamma) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones (TZDs), a group of structurally related synthetic agonists with antidiabetic actions in vivo. Rosiglitazone (BRL49653) is a prototypical TZD and has...