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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1239578-79-0
- 分子式: C21H14N4O3S
- 分子量:402.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1239578-79-0
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分子量 402.43
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分子式 C21H14N4O3S
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SMILES
O=C1NC2=C(N(C(C1)=O)C3=CC=CC(C4=NOC(N4)=S)=C3)C=CC5=C2C=CC=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)