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PSB 1114

Names

[ CAS No. ]:
1657025-60-9

[ Name ]:
PSB 1114

Biological Activity

[Description]:

PSB-1114 tetrasodium is a potent, enzymatically stable, and subtype-selective P2Y2 receptor agonist with an EC50 of 134 nM. PSB-1114 tetrasodium displays >50-fold selectivity versus the P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors[1].

[Related Catalog]:

Research Areas >> Others
Signaling Pathways >> GPCR/G Protein >> P2Y Receptor

[Target]

EC50: 134 nM (P2Y2 receptor), 9.3 μM (P2Y4 receptor); 7.0 μM (P2Y6 receptor)[1]


[In Vitro]

PSB-1114 (4-Thio-β,γ-difluoromethylene-UTP; compound 14g) displays >60-fold selectivity versus P2Y4 and P2Y6 receptors. Because of its high potency, selectivity, and expected metabolic stability toward ectonucleotidases, in particular NTPDases, PSB-1114 may be a useful pharmacological tool for studying P2Y2 receptors[1].

[References]

[1]. El-Tayeb A, et al. Structural modifications of UMP, UDP, and UTP leading to subtype-selective agonists for P2Y2, P2Y4, and P2Y6 receptors. J Med Chem. 2011 Apr 28;54(8):2878-90.

[2]. Rafehi M, et al. Tools and drugs for uracil nucleotide-activated P2Y receptors. Pharmacol Ther. 2018 Oct;190:24-80.

Chemical & Physical Properties

[ Molecular Formula ]:
C10H11F2N2Na4O13P3S

[ Molecular Weight ]:
622.14

Related Compounds