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

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2728291-29-8
• MW: 346.18
• Purity: 98.88% (May vary between batches)
• Formula: C₁₅H₁₂BrN₃O₂
• SMILES: O=C(NC=1C=CC=2N=CNC2C1)COC3=CC=C(Br)C=C3
• Target: NOD-like Receptor (NLR),P2Y Receptor
• Solubility: DMSO:40 mg/mL (115.55 mM)

Bioactivity

• 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

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Compound Identifiers

PubChem CID

166194091