Shopping Cart
- Remove All
- Your shopping cart is currently empty
P2Y14R antagonist 1 (compound I-17) is a selective and potent P2Y14R antagonist (IC50=0.6 nM) with oral activity and good bioavailability that inhibits monosodium urate-induced inflammatory response in acute gouty arthritis by reducing inflammatory factor release via the NLRP3/GSDMD signaling pathway and cellular pyroptosis.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $42 | In Stock | |
5 mg | $98 | In Stock | |
10 mg | $156 | In Stock | |
25 mg | $313 | In Stock | |
50 mg | $493 | In Stock | |
100 mg | $786 | In Stock |
Description | P2Y14R antagonist 1 (compound I-17) is a selective and potent P2Y14R antagonist (IC50=0.6 nM) with oral activity and good bioavailability that inhibits monosodium urate-induced inflammatory response in acute gouty arthritis by reducing inflammatory factor release via the NLRP3/GSDMD signaling pathway and cellular pyroptosis. |
Targets&IC50 | P2Y14R (HEK293 cells):0.11 nM (Kᴅ), P2Y14R (HEK293 cells):0.60 nM |
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[1]. 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[1]. |
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[1]. |
Molecular Weight | 346.18 |
Formula | C15H12BrN3O2 |
Cas No. | 2728291-29-8 |
Smiles | O=C(NC=1C=CC=2N=CNC2C1)COC3=CC=C(Br)C=C3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40 mg/mL (115.55 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
|
Copyright © 2015-2025 TargetMol Chemicals Inc. All Rights Reserved.