PSB 0474 

PSB 0474 (3-phenacyl-UDP) is a UDP (HY-113359) analog and selective P2Y₆ receptor agonist, with an EC₅₀ value of 70 nM for the hP2Y₆ receptor. PSB 0474 activates Phospholipase C-coupled receptors to increase intracellular inositol phosphate levels. PSB 0474 enhances NO release by upregulating inducible iNOS and induces Apoptosis. PSB 0474 increases micturition frequency in urine of anesthetized rats, without altering bladder contraction amplitude/duration or causing urothelial damage. PSB 0474 can be used in studies related to chronic brain inflammation^[1][2][3].

PSB 0474 (1-100 µM; 10 min) acts as a weak agonist of the hP2Y₂ receptor expressed in 1321N1 astrocytoma cells, with an estimated EC₅₀ of approximately 40000 nM^[1].
PSB 0474 (100 µM; 10 min) is a very weak agonist of the hP2Y₄ receptor expressed in 1321N1 astrocytoma cells, with an EC₅₀ >100000 nM^[1].
PSB 0474 (10 min) is a potent full agonist of the hP2Y₆ receptor expressed in 1321N1 astrocytoma cells, with an EC₅₀ of 70 nM, and shows approximately 500-fold higher selectivity for the P2Y₆ receptor over the P2Y₂ and P2Y₄ receptors^[1].
PSB 0474 (0.01-10 μM; 48 h) potently inhibits microglial proliferation by activating microglial P2Y₆ receptors coupled to the Gq-PLC-PKC signaling pathway^[2].
PSB 0474 (10 μM; 48 h) increases nitric oxide release to 199% by activating microglial P2Y₆ receptors coupled to the PLC-PKC pathway, and iNOS is upregulated exclusively in microglia^[2].
PSB 0474 (10 μM; 48 h) selectively induces apoptosis in astrocytes without affecting the viability of microglia^[2].

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

PSB 0474 (100 nM; intravesical infusion) activates P2Y₆ receptors to increase voiding frequency in anaesthetized rats by releasing ATP from the urothelium, with no effect on voiding contraction amplitude or duration^[3].

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

522.29

C₁₇H₂₀N₂O₁₃P₂

917567-60-3

O[C@H]([C@@H]1O)[C@@](N(C=CC2=O)C(N2CC(C3=CC=CC=C3)=O)=O)([H])O[C@@H]1CO[P](O[P](O)(O)=O)(O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. El-Tayeb A, et al. Synthesis and structure-activity relationships of uracil nucleotide derivatives and analogues as agonists at human P2Y2, P2Y4, and P2Y6 receptors. J Med Chem. 2006;49(24):7076-7087.  [Content Brief]

  [2]. Quintas C, et al. Microglia P2Y₆ receptors mediate nitric oxide release and astrocyte apoptosis. J Neuroinflammation. 2014;11:141. Published 2014 Sep 3.  [Content Brief]

  [3]. Carneiro I, et al. Activation of P2Y6 receptors increases the voiding frequency in anaesthetized rats by releasing ATP from the bladder urothelium. Br J Pharmacol. 2014;171(14):3404-3419.