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.
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- CAS No.: 917567-60-3
- 화학식: C17H20N2O13P2
- 분자량:522.29
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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P2Y6 Receptor 70 nM (EC50) |
PLC |
iNOS |
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.
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Cell Line:microglial
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Concentration:0.01-10 μM
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Incubation Time:48 h
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Result:Inhibited microglial proliferation with a maximum inhibition rate of 43%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (male, 300-450 g, urethane-anaesthetized)[3]
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Dosage:100 nM
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Administration:intravesical infusion
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Result:Decreased intercontraction interval, increasing voiding frequency to a similar extent as 100 μM UDP.
Did not significantly affect amplitude or duration of voiding bladder contractions.
Increased ATP levels in voided cystometry fluid by more than threefold (from ~10 nM to ~37 nM).
Caused no significant change in LDH activity in voided fluid.
Chemical Information
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CAS No. 917567-60-3
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분자량 522.29
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화학식 C17H20N2O13P2
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SMILES
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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PSB 0474 Related Classifications
HY-108654 Related Classifications
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