a3ar

Compound 15A, also known as A3AR agonist 3, acts as an agonist for the A3 adenosine receptor (A3AR), exhibiting K_i and EC_50 values of 2.27 nM and 0.20 nM for hA3 and cAMP, respectively. This compound is utilized in neuroinflammation research [1].

A3AR agonist 4, an A3 adenosine receptor (A3AR) agonist, exhibits an inhibitory affinity (K i) of 1.24 nM for hA3AR and dampens cAMP production with an EC 50 value of 0.17 nM. It is utilized in the study of inflammation and pain [1].

Compound 6b, also known as A3AR agonist 5, serves as an A3 adenosine receptor (A3AR) activator and exhibits potent EC50 and Ki values of 0.14 nM and 6.36 nM for cAMP and hA3, respectively. This compound is primarily utilized in research related to pain and inflammation [1].

A3AR antagonist 2 is a potent antagonist of the human A3 adenosine receptor, exhibiting a Ki value of 4.54 nM.

A3AR modulator 1 (MRS8054), an orally active positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR) (Adenosine Receptor), significantly enhances the efficacy (E max) of Cl-IB-MECA-stimulated [35 S]GTPγS binding [1].

A3AR antagonist 1 is a potent and selective human A3adenosine receptor (AR) antagonist (Ki: 4.63) and has no affinity for the rat A3AR.

A3AR Agonist 1 (Compound 12), with a Ki of 25.8 nM, is a potent A3 adenosine receptor (A3AR) agonist that promotes β-arrestin2 recruitment with an effective concentration (EC50) of 5.17 nM. It serves as a research tool in various pathological conditions, including inflammatory diseases, ischemia, cancer, neuropathic pain, and liver diseases [1].

Compound 19, a selective A3 Adenosine Receptor (A3AR) agonist (K i : 22.1 nM), effectively stimulates β-arrestin2 recruitment with an EC 50 value of 4.36 nM. This compound is utilized in research pertaining to inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, and other chronic conditions [1].

A1/A3 AR Antagonist 3 is a dual A1R/A3R antagonist that demonstrates high affinity within the low-micromolar to nanomolar range, and is potentially useful in the research of chronic heart diseases [1].

When administered intratumorally, AR antagonist 3 shows effective inhibition on the growth of tumor. AR antagonist 3 is a potent and selective antagonist of androgen receptor (AR) with an IC 50 of 0.47 μM. AR antagonist 3 dose-dependently decrease the FRET signal with an IC50 of 18.05 μM [1].

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.

hA3AR agonist 1 is a potent human A3 adenosine receptor (hA3AR) agonist with a Ki of 2.40 nM.

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

N6-Ethyladenosine, an adenosine derivative, acts as an agonist of Adenosine receptors (hA1AR and hA3AR) with Ki values of 4.9 nM and 4.7 nM, respectively.

MRS1186 is an effective and selective antagonist of the human Adenosine A3 receptor (Ki: 7.66 nM).

MRS 5980, an A3AR agonist with a K i value of 0.7 nM, exhibits oral activity [1].

MRS542 is a A3AR antagonist as found by cyclic AMP assays, and a partial agonist as found by beta-arrestin translocation. LUF6000 is responsible for the partial agonist nature of MRS542.

PSB-10 hydrochloride is a human adenosine A3 receptor antagonist.

MRS1177 is an effective and selective antagonist of the human Adenosine A3 receptor (hA3AR) (Ki: 0.3 nM).

DPTN dihydrochloride is a potent and selective A3AR antagonist with Ki values of 1.65, 9.61 and 8.53 nM in human, mouse and rat, respectively.