53 products were found matching "K04267"!

PSB-603 is an antagonist of the adenosine A2B receptor (Ki = 0.553 nM). It is selective for adenosine A2B over A1, A2A, and A3 receptors (Kis = >10,000 nM). It reduces intracellular calcium concentrations in Jurkat T cells expressing the human A2B receptor (IC50 = 1.13 nM). PSB-603 reduces Zika viral plaque...

Description: MPO-IN-28 is a novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM. Target: Glutathione Peroxidase. Smiles: COc1ccc2c(C)nc(NC(N)=N)nc2c1. References: Soubhye J, et al. Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening...

Description: PSB-1115 potassium salt, a selective A2B Adenosine Receptor antagonist, inhibits the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced contraction inhibition of acetylcholine (ACh) [1]. Target: Others. Smiles: O=C1C2=C(N=C(N2)C3=CC=C(S(=O)(=O)O)C=C3)NC(=O)N1CCC.[K]

Description: BAY-545 is an antagonist of A2B adenosine receptor(IC50 : 59 nM). Target: Adenosine Receptor. Smiles: CCn1c(=O)n(CCC(F)(F)F)c2sc(C(=O)N3CCC(O)CC3)c(C)c2c1=O. References: Härter M, et al. Novel non-xanthine antagonist of the A2B adenosine receptor: From HTS hit to lead structure. Eur J Med Chem. 2019 Feb...

Description: BAY 60-6583 is a potent, high-affinity adenosine A2B receptor agonist (EC50 = 3 nM) with affinity for A2B receptors that exceeds that for A1, A2A, and A3 receptors.BAY 60-6583 is cardioprotective in a model of myocardial ischemia.The Ki values for BAY 60-6583 binding to mouse, rabbit, and dog A2BAR were...

Description: MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1, and A3 receptors respectively. MRS-1706 is an effective and selective adenosine A2B receptor inverse agonist. Target: Adenosine Receptor. Smiles: CCCn1c2[nH]c(nc2c(=O)n(CCC)c1=O)-c1ccc(OCC(=O)Nc2ccc(cc2)C(C)=O)cc1. References:...

Description: MRS 1754 is a selective antagonist radioligand for the A2B adenosine receptor, exhibiting very low affinity for A1 and A3 receptors in both humans and rats. Target: Adenosine Receptor. Smiles: CCCn1c2[nH]c(nc2c(=O)n(CCC)c1=O)-c1ccc(OCC(=O)Nc2ccc(cc2)C#N)cc1. References: Ji X, et al. [3H]MRS 1754, a...

Description: GS-6201 (CVT-6883) is a selective antagonist of the adenosine A2B receptor, demonstrating high affinity and selectivity with a Ki of 22 nM for human adenosine A2B receptors. Target: Adenosine Receptor. Smiles: CCCn1c(=O)n(CC)c2[nH]c(nc2c1=O)-c1cnn(Cc2cccc(c2)C(F)(F)F)c1. References: Toldo S, et al....

BAY 60-6583 is an adenosine A2B receptor agonist (EC50 = 3 nM for human A2B receptors) that displays selectivity over A1, A2A, and A3 receptors (EC50s = >10 µM). It has been used to decrease superoxide production in neutrophils and to study the role of the A2B receptor in regulating inflammation and mediating...

Adenosine is a purine nucleoside composed of adenine and ribose linked by a glycosidic linkage. It is an endogenous ligand of a family of four adenosine receptors, which serve diverse roles related to smooth muscle tone, central nervous system regulation, and cardiac function. Adenosine is a precursor for adenosine...

PSB-1115 is an antagonist of the adenosine A2B receptor (Ki = 53.4 nM). It is selective for A2B over A1 and A2A receptors, which have Ki values of 2,200 and 24,000 nM, respectively, and over the A3 receptor, which it inhibits only 14% at a concentration of 10 µM. PSB-1115 pre-treatment reduces relaxation of rat...

Picotamide is an antiplatelet drug that inhibits both thromboxane A2 (TXA2) receptors (Kd = 325 nM) and TXA2 synthase. It significantly inhibits basal and lipopolysaccharide-stimulated TXA2 synthesis by rat peritoneal macrophages when used at 0.5 mM. Formulations containing picotamide have potential applications in...