NP-1815-PX 

NP-1815-PX is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC₅₀ of 0.26 μM against human P2X4 receptors. NP-1815-PX specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX is used in studies related to asthma and inflammatory bowel disease (colitis)^[1][2].

NP-1815-PX (10^-5 M; 30 min) strongly suppresses ATP-induced contractions in guinea pig epithelium-intact tracheal smooth muscle^[1].
NP-1815-PX (10^-5-10^-4 M; 60 min) inhibits U46619-induced contractions in a concentration-dependent manner in guinea pig epithelium-denuded tracheal smooth muscle, with an apparent pA₂ value of 4.59^[1].
NP-1815-PX (10^-5-10^-4 M; 60 min) inhibits PGF₂α-induced contractions in a concentration-dependent manner in guinea pig epithelium-denuded tracheal smooth muscle^[1].
NP-1815-PX (10^-4 M; 60 min) does not substantially inhibit contractions induced by carbachol, histamine, neurokinin A, or 50 mM KCl in guinea pig epithelium-denuded tracheal smooth muscle^[1].
NP-1815-PX (10^-5-10^-4 M; 60 min) inhibits U46619-induced contractions in a concentration-dependent manner in guinea pig epithelium-denuded bronchial smooth muscle^[1].
NP-1815-PX (10^-5-10^-4 M; 10 min) inhibits TP receptor-expressing 293T cells-induced intracellular Ca²⁺ increases in a concentration-dependent manner in human TP receptor-expressing 293T cells^[1].
NP-1815-PX (0.1-10 μM; 1 h pre-incubation) modulates canonical and non-canonical NLRP3 inflammasome pathways in human monocytic THP-1 cells, with 10 μM significantly reducing LPS/ATP-induced NLRP3, cleaved caspase-1, caspase-5, and caspase-8 expression, as well as IL-1β release^[2].

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

NP-1815-PX (3-30 mg/kg; p.o.; daily; 6 days) significantly attenuates DNBS (HY-W324435)-induced body weight loss, spleen weight increase, and macroscopic colonic injury in rats, with the 10 mg/kg dose additionally significantly reducing colonic caspase-1 activity and restoring occludin expression, while none of the doses significantly reduce microscopic colonic damage or DNBS-induced colonic IL-1β increases^[2].

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

402.43

C₂₁H₁₄N₄O₃S

1239578-79-0

O=C1NC2=C(N(C(C1)=O)C3=CC=CC(C4=NOC(N4)=S)=C3)C=CC5=C2C=CC=C5

Room temperature in continental US; may vary elsewhere.

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

• [1]. Obara K, et al. Effects of NP-1815-PX, a P2X4 Receptor Antagonist, on Contractions in Guinea Pig Tracheal and Bronchial Smooth Muscles. Biol Pharm Bull. 2022;45(8):1158-1165.  [Content Brief]

  [2]. D’Antongiovanni V, et al. RETRACTED ARTICLE: Anti-inflammatory Effects of Novel P2X4 Receptor Antagonists, NC-2600 and NP-1815-PX, in a Murine Model of Colitis[J]. Inflammation, 2022, 45(4): 1829-1847.