Art. -Nr.: HY-150270A

NP-1815-PX sodium

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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).

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Reinheit: 99.51%
CAS. Nr.: 1239578-80-3
Formel: C₂₁H₁₃N₄NaO₃S
Molecular Weight:424.41

Speicherung:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

NP-1815-PX sodium Chemical Structure

CAS. Nr.: 1239578-80-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Caspase-1

IL-1β

P2X4 Receptor

Alle P2X Receptor Isoform-spezifische Produkte anzeigen :

Alle Prostaglandin Receptor Isoform-spezifische Produkte anzeigen :

Alle NOD-like Receptor (NLR) Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Alle Interleukin Related Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Western Blot Analysis^[2]

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.

In Vivo

NP-1815-PX (3-30 mg/kg; p.o.; daily; 6 days) sodium 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.

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

CAS. Nr. 1239578-80-3
Appearance Solid
Molecular Weight 424.41
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3562 mL

11.7811 mL

23.5621 mL

5 mM

0.4712 mL

2.3562 mL

4.7124 mL

10 mM

0.2356 mL

1.1781 mL

2.3562 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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NP-1815-PX sodium

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Alle P2X Receptor Isoform-spezifische Produkte anzeigen

Alle Prostaglandin Receptor Isoform-spezifische Produkte anzeigen

Alle NOD-like Receptor (NLR) Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Alle Interleukin Related Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NP-1815-PX sodium Related Classifications

HY-150270A Related Classifications