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P2Y14R antagonist 1

SKU: orb2646171

Description

P2Y14R antagonist 1 (I-17) is a potent, selective, and orally bioavailable antagonist of the P2Y14 receptor (IC50=0.6 nM). It suppresses monosodium urate-induced inflammation in acute gout models by targeting the NLRP3/GSDMD pathway to inhibit pyroptosis and inflammatory cytokine release, making it a valuable tool for studying purinergic signaling in inflammatory diseases.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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P2Y14R antagonist 1

Key Properties

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CAS Number2728291-29-8
MW346.18
Purity98.88% (May vary between batches)
FormulaC15H12BrN3O2
SMILESO=C(NC=1C=CC=2N=CNC2C1)COC3=CC=C(Br)C=C3
TargetP2Y Receptor,NOD-like Receptor (NLR)
SolubilityDMSO:40 mg/mL (115.55 mM)

Bioactivity

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Target IC50
P2Y14 receptor (HEK293 cells):0.11 nM (Kᴅ)|P2Y14 receptor (HEK293 cells):0.60 nM
In Vivo
P2Y14R antagonist 1（compound I-17）exhibited good oral bioavailability (F = 75%) in rats (20 mg/kg, p.o., T₁/₂ = 12.6 h). In an MSU-induced mouse model of acute gouty arthritis, P2Y14R antagonist 1 effectively reduced paw swelling, downregulated pro-inflammatory cytokines (IL-1β, IL-6, IL-18), attenuated immune cell infiltration and joint histopathological damage, and decreased NLRP3 expression.
In Vitro
P2Y14R antagonist 1 （Compound I-17）showed potent inhibition of P2Y14R in HEK293 cells (IC₅₀ = 0.60 nM; K_D = 0.11 nM) and had no significant effect on other P2Y receptors. In RAW264.7 cells, P2Y14R antagonist 1 (10–40 μM) inhibited MSU+LPS-induced IL-1β, IL-6, and IL-18 release, reduced NLRP3 and GSDMD expression, and suppressed pyroptosis.

Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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Quality Guarantee

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Compound Identifiers

PubChem CID
166194091 ↗

Key Properties

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No computed properties available.

Protocol Information

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1 mg
$ 90.00
5 mg
$ 140.00
10 mg
$ 200.00
25 mg
$ 360.00
50 mg
$ 540.00
100 mg
$ 830.00
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