380221-63-6

380221-63-6 structure

Name: UK-432097
Chemical Name: 6-(2,2-diphenylethylamino)-9-[(2R,3R,4S,5S)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-N-[2-[(1-pyridin-2-ylpiperidin-4-yl)carbamoylamino]ethyl]purine-2-carboxamide
CAS Number: 380221-63-6
Molecular Formula: C₄₀H₄₇N₁₁O₆
Molecular Weight: 777.87
Catalog: Signaling Pathways GPCR/G Protein Adenosine Receptor
Create Date: 2016-02-13 00:12:05
Modify Date: 2024-01-11 00:31:37
UK-432097 is a highly potent and selective A2AAR agonist with a pKi of 8.4 for human A2AAR. UK-432097 has anti-inflammatory and anti-aggregatory properties. UK-432097 has the potential for COPD (Chronic Obstructive Pulmonary Disease) research[1][2][3].

Name	6-(2,2-diphenylethylamino)-9-[(2R,3R,4S,5S)-5-(ethylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]-N-[2-[(1-pyridin-2-ylpiperidin-4-yl)carbamoylamino]ethyl]purine-2-carboxamide
Synonyms	3qak 6-[(2,2-Diphenylethyl)amino]-9-{(2R,3R,4S,5S)-5-[(ethylamino)carbonyl]-3,4-dihydroxytetrahydro-2-furanyl}-N-(2-[({[1-(2-pyridinyl)-4-piperidinyl]amino}carbonyl)amino]ethyl)-9H-purine-2-carboxamide UNII-8L3OAJ1R5A UK-432,097 6-(2,2-Diphenylethylamino)-9-[(2r,3r,4s,5s)-5-(Ethylcarbamoyl)-3,4-Dihydroxy-Oxolan-2-Yl]-N-[2-[(1-Pyridin-2-Ylpiperidin-4-Yl)carbamoylamino]ethyl]purine-2-Carboxamide

Description	UK-432097 is a highly potent and selective A2AAR agonist with a pKi of 8.4 for human A2AAR. UK-432097 has anti-inflammatory and anti-aggregatory properties. UK-432097 has the potential for COPD (Chronic Obstructive Pulmonary Disease) research[1][2][3].
Related Catalog	Research Areas >> Inflammation/Immunology Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor
Target	pKi: 8.4 (A2AAR)[1]
In Vitro	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].
References	[1]. Fei Xu, et al. Structure of an agonist-bound human A2A adenosine receptor. Science. 2011 Apr 15;332(6027):322-7. [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. [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.