a3

Fostamatinib (R788) is a small-molecule inhibitor and an oral prodrug of R406, a Syk/FLT3-targeted inhibitor (IC50 = 41 nM) that also inhibits Lyn (IC50 = 63 nM) and Lck (IC50 = 37 nM), featuring oral activity and cell permeability, used for the treatment of immune thrombocytopenia.

N6-(2-Phenylethyl)adenosine (N6-Phenethyladenosine) is an adenosine derivative and adenosine receptor agonist with Ki values of 11.8 nM for rat A1 receptors and 30.1 nM for human A1 receptors.

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 750 nM, 340 nM, and 330 nM, respectively. The Ki values of BAY 60-6583 binding to A2BAR in mice, rabbits and dogs were 750 nM, 340 nM and 330 nM respectively.

Acefylline (Theophylline-7-acetic acid), a stimulant drug of the xanthine chemical class, acts as an adenosine receptor antagonist. It is combined with diphenhydramine in the pharmaceutical preparation Etanautine to help offset its stimulant effects

CHEMBL241987 targets the Adenosine receptor A3 (human)

MRS-3777 hemioxalate, a selective adenosine A3 receptor antagonist, reverses the anti-injury perception effects of its corresponding agonist and serves as a valuable tool for studying inflammatory pain.

APNEA ((2R,3R,4S,5R)-2-[6-[2-(4-aminophenyl)ethylamino]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol) is a non-selective agonist of adenosine A3 receptor.

CGS 15943 is an orally bioavailable non-xanthine antagonist of the Adenosine Receptor. In transfected CHO cells, its Ki values for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM, respectively.

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.

N6-Cyclopentyladenosine (CPA) is a selective agonist of the adenosine A1 receptor, mimicking its action with Ki values of 2.3 nM, 790 nM, and 43 nM for human A1, A2A, and A3 receptors, respectively. CPA is used to modulate cellular signaling, neurotransmission, and other biological processes.

Reversine, a small synthetic purine analogue (2, 6-disubstituted purine), is a potent inhibitior of Aurora A/B/C(IC50s=150-500 nM).

MRS1220, a selective and potent antagonist for the human A3 adenosine receptor (hA3AR) with a dissociation constant (Ki) of 0.59 nM, exhibits therapeutic promise for central nervous system disease research. It effectively diminishes glioblastoma tumor size and inhibits blood vessel formation in vivo.

VUF 5574 is a selective antagonist of adenosine A3 receptor with a Ki of 4.03 nM for the recombinant human receptor.

Vipadenant (CEB-4520)(BIIB-014) is an adenosine A2a antagonist with Ki of 1.3 nM; less potent for A1(Ki=69 nM).

Namodenoson (2-Cl-IB-MECA) is an adenosine A3 receptor agonist.

Piclidenoson (CF-101), a selective agonist of adenosine A3 receptor(EC50 values of 0.11 μM), induces robust anti-inflammatory effect in psoriasis patients.

Chromomycin A3 is an antibiotic produced by Streptomyces sp that binds to gc-rich DNA sequences in the presence of divalent cations and inhibits DNA replication and transcription; it is also used as a fluorescent DNA stain and assay; and it has anticancer activity against diseases such as Hodgkin's, lung adenocarcinomas, melanomas, and breast cancer.

Isogibberellin A3 is a useful organic compound for research related to life sciences. The catalog number is T125477 and the CAS number is 19123-67-2.

Sibiricose A3 is a compound isolated from the roots of Polygala sibirica L. It is used in the study of prostate cancer.

Milbemycin A3 Oxime is a macrolide antiparasitic agent that exhibits potent inhibitory activity against Dirofilaria immitis.

Prostaglandin A3 is a non-enzymatic dehydration product of prostaglandin E3 (PGE3). It demonstrates significant affinity for canine EP2 and EP4 receptors with IC50 values of 120 nM and 20 nM, respectively. For human PPARγ, Prostaglandin A3 has a Ki value of 188 μM.

Hepoxilin A3 methyl ester is the ester form of HxA3. It effectively induces the release of intracellular calcium ions, subsequently facilitating calcium influx in suspended human neutrophils.

Hepoxilin A3 (HXA3) is a neutrophil chemoattractant synthesized through the activation of the PLA2-12-LOX pathway. It directs neutrophils to migrate across epithelial barriers to sites of infection, such as the alveolar space. In mouse models, levels of Hepoxilin A3 rise in tandem with neutrophil infiltration. It is used in research on inflammatory diseases like pneumonia and cystic fibrosis.

A2A/A3 agonist-1 serves as a dual A2A/A3 adenosine receptor agonist. It has a Ki value greater than 2.9 nM and an EC50 of 0.51 nM for hA2AAR. For hA3AR, the Ki is 0.8 nM and the EC50 is less than 0.10 nM. A2A/A3 agonist-1 exhibits anti-inflammatory properties and is applicable in the research of inflammatory diseases.