2. Membrane Transporter/Ion Channel GPCR/G Protein Immunology/Inflammation Apoptosis
  3. P2X Receptor Prostaglandin Receptor NOD-like Receptor (NLR) Caspase Interleukin Related
  4. NP-1815-PX sodium

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).

For research use only. We do not sell to patients.

NP-1815-PX sodium

NP-1815-PX sodium Chemical Structure

CAS No. : 1239578-80-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of NP-1815-PX sodium:

NP-1815-PX sodium Related Antibodies

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P2X1 Receptor P2X2 Receptor P2X3 Receptor P2X4 Receptor P2X7 Receptor

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DP EP FP IP TXA2/TP TXB2

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NLRP3 NLRP1 NOD1 NOD2

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

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)[1][2].

IC50 & Target

Caspase-1

 

IL-1β

 

TP

 

P2X4 Receptor

 

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.

NP-1815-PX sodium Related Antibodies

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).
Molecular Weight

424.41

Formula

C21H13N4NaO3S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3562 mL 11.7811 mL 23.5621 mL
5 mM 0.4712 mL 2.3562 mL 4.7124 mL
View the 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.

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Purity & Documentation
References

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
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NP-1815-PX sodium Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NP-1815-PX1239578-80-3P2X ReceptorProstaglandin ReceptorNOD-like Receptor (NLR)CaspaseInterleukin RelatedP2XRsILmiceprostanoid TP receptorNLRP3 inflammasomeguinea pig tracheal smooth muscleTHP-1 cells293T cellsguinea pig bronchial smooth muscleSprague-Dawley ratsP2X4 receptorsmooth muscleInhibitorinhibitorinhibit

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