human a2b receptor

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.

human A2B adenosine receptor antagonist

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.

AMP-579 is an adenosine A1 receptor agonist. AMP-579 also acts as a A2b-adenosine receptor agonist in human 293 cells and rabbit hearts.

Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR), exhibiting exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties, holding great promise for investigating cancer and neurodegenerative diseases [1].

Adenosine receptor inhibitor 2 (compound 14b) is a potent inhibitor of AR (adenosine receptor), exhibiting dual affinity towards A1 A2A ARs with higher affinity for A1- than A2A AR, and Ki values of 52.2 nM for A1 AR and 167 nM for A2A AR.

A2AAR HDAC-IN-1 (compound 14c) is an orally active, balanced dual inhibitor of A2AAR (Ki: 163.5 nM) and HDAC1 (IC50: 145.3 nM).

PSB-1901 is a potent A2B Adenosine Receptor Antagonist with Picomolar Potency (Ki 0.0835 nM, KB 0.0598 nM, human A2BAR) with >10 000-fold selectivity versus all other AR subtypes. PSB-1901 was similarly potent and selective at the mouse A2BAR, making it a promising tool for preclinical studies.