UK-432097 

UK-432097 is a highly potent and selective A_2AAR agonist with a pK_i of 8.4 for human A_2AAR. UK-432097 has anti-inflammatory and anti-aggregatory properties. UK-432097 has the potential for COPD (Chronic Obstructive Pulmonary Disease) research^[1][2][3].

pKi: 8.4 (A2AAR)^[1]

UK-432097 has an EC₅₀ value of 0.66 nM using CHO cells expressing human WT A₅₀AR^[1].
UK-432097 (0.01, 0.1, 1, 10, 100, 1000 nM; pretreated for 2 hours) significantly increases cAMP accumulation in CHO-A2A cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

777.87

C₄₀H₄₇N₁₁O₆

380221-63-6

Solid

White to off-white

O[C@H]1[C@@H](O[C@H](C(NCC)=O)[C@H]1O)N2C3=NC(C(NCCNC(NC4CCN(C5=CC=CC=N5)CC4)=O)=O)=NC(NCC(C6=CC=CC=C6)C7=CC=CC=C7)=C3N=C2

Room temperature in continental US; may vary elsewhere.

• [1]. Fei Xu, et al. Structure of an agonist-bound human A2A adenosine receptor. Science. 2011 Apr 15;332(6027):322-7.  [Content Brief]

  [2]. Kenneth A Jacobson, et al. Historical and Current Adenosine Receptor Agonists in Preclinical and Clinical Development. Front Cell Neurosci. 2019 Mar 28;13:124.  [Content Brief]

  [3]. J Daniel Hothersall, et al. Structure-Activity Relationships of the Sustained Effects of Adenosine A2A Receptor Agonists Driven by Slow Dissociation Kinetics. Mol Pharmacol. 2017 Jan;91(1):25-38.  [Content Brief]