NP-1815-PX sodium
Based on 1 Customer Validation
NP-1815-PX sodium 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 sodium specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX sodium selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX sodium 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 sodium exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX sodium is used in studies related to asthma and inflammatory bowel disease (colitis).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.51%
- No. CAS: 1239578-80-3
- Fòrmula: C21H13N4NaO3S
- Peso molecular:424.41
-
Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas P2X Receptor
MoreVer todos los productos específicos de isoformas Caspase
More
Actividad biológica
|
Caspase-1 |
IL-1β |
TP |
P2X4 Receptor |
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.
-
Cell Line:Human monocytic THP-1 cells
-
Concentration:10 µM
-
Incubation Time:1 h pre-incubation
-
Result:Significantly reduced the levels of LPS/ATP-induced NLRP3, cleaved caspase-1, caspase-5, and caspase-8 expression, as well as IL-1β release in human monocytic THP-1 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Sprague-Dawley (male, 200-225 g body weight, DNBS-induced colitis)[2]
-
Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
-
Administration:p.o.; daily; 6 days
-
Result:Attenuated DNBS-induced body weight loss.
Counteracted DNBS-induced spleen weight increase.
Significantly reduced macroscopic colonic injury score.
Significantly reduced DNBS-induced colonic caspase-1 activity (10 mg/kg dose).
Significantly restored colonic occludin expression.
Did not significantly reduce DNBS-induced microscopic colonic damage (all doses).
Counteracted, though not significantly, DNBS-induced colonic IL-1β increases (all doses); did not significantly reduce DNBS-induced colonic TNF increases (all doses).
Chemical Information
-
No. CAS 1239578-80-3
-
Appearance Solid
-
Peso molecular 424.41
-
Fòrmula C21H13N4NaO3S
-
Color White to off-white
-
SMILES
O=C1NC2=C(N(C(C1)=O)C3=CC=CC(C4=NOC(N4[Na])=S)=C3)C=CC5=C2C=CC=C5
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : 250 mg/mL (589.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
-
Ficha de datos (286 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3562 mL | 11.7811 mL | 23.5621 mL | 58.9053 mL |
| 5 mM | 0.4712 mL | 2.3562 mL | 4.7124 mL | 11.7811 mL | |
| 10 mM | 0.2356 mL | 1.1781 mL | 2.3562 mL | 5.8905 mL | |
| 15 mM | 0.1571 mL | 0.7854 mL | 1.5708 mL | 3.9270 mL | |
| 20 mM | 0.1178 mL | 0.5891 mL | 1.1781 mL | 2.9453 mL | |
| 25 mM | 0.0942 mL | 0.4712 mL | 0.9425 mL | 2.3562 mL | |
| 30 mM | 0.0785 mL | 0.3927 mL | 0.7854 mL | 1.9635 mL | |
| 40 mM | 0.0589 mL | 0.2945 mL | 0.5891 mL | 1.4726 mL | |
| 50 mM | 0.0471 mL | 0.2356 mL | 0.4712 mL | 1.1781 mL | |
| 60 mM | 0.0393 mL | 0.1964 mL | 0.3927 mL | 0.9818 mL | |
| 80 mM | 0.0295 mL | 0.1473 mL | 0.2945 mL | 0.7363 mL | |
| 100 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5891 mL |
NP-1815-PX sodium Related Classifications
HY-150270A Related Classifications
Powered by Bioz
- NP-1815-PX
- 1239578-80-3
- P2X Receptor
- Prostaglandin Receptor
- NOD-like Receptor (NLR)
- Caspase
- Interleukin Related
- mice
- prostanoid TP receptor
- NLRP3 inflammasome
- guinea pig tracheal smooth muscle
- THP-1 cells
- 293T cells
- guinea pig bronchial smooth muscle
- Sprague-Dawley rats
- P2X4 receptor
- smooth muscle
- Inhibitor
- inhibitor
- inhibit