| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
NP-1815-PX sodium selectively targets the P2X4 purinergic receptor (P2X4R), a ligand-gated ion channel involved in neuroinflammation and chronic pain signaling. It shows high potency for human P2X4 with an IC50 of 0.26 uM. It also exhibits secondary antagonistic activity at the thromboxane A2 (TP) receptor. NP-1815-PX sodium is highly selective for P2X4R over other P2X receptor subtypes.
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| ln Vitro |
In vitro, NP-1815-PX sodium blocks ATP-evoked currents in cells expressing P2X4 receptors, with an IC50 of approximately 0.26 uM for the human P2X4 receptor. It demonstrates potent and selective antagonism, with minimal activity at other P2X subtypes. The compound is also effective at inhibiting guinea pig tracheal and bronchial smooth muscle contractions, underscoring its potential in respiratory and pain research.
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| ln Vivo |
In vivo, NP-1815-PX sodium exhibits anti-allodynic effects in mouse models of chronic pain. Intrathecal administration produces pain relief in mice with traumatic nerve damage without affecting acute nociceptive pain or motor function. The compound also shows anti-inflammatory activity and can be used in chronic pain models, including neuropathic and inflammatory pain, to study P2X4R-mediated pain signaling.
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| Enzyme Assay |
For in vitro P2X4R antagonism assays, HEK293 cells stably expressing human P2X4 receptors are loaded with a calcium-sensitive dye. Cells are pre-incubated with NP-1815-PX sodium at increasing concentrations (0.01-10 uM) for 5-10 minutes. ATP (typically 10-100 uM) is then added to activate the receptor, and calcium influx is measured by fluorescence change. IC50 values are calculated using dose-response curve fitting.
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| Cell Assay |
For cell-based assays, primary microglia or P2X4-expressing cell lines are treated with NP-1815-PX sodium at concentrations ranging from 0.1-10 uM for 30-60 minutes, then stimulated with ATP (100 uM) to activate P2X4 receptors. P2X4-mediated calcium influx is measured using Fluo-4 or Fura-2 dyes. Supernatants can be collected to measure pro-inflammatory cytokines (e.g., IL-1beta, TNF-alpha) by ELISA. Viability is assessed by MTT or ATP-based assays.
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| Animal Protocol |
For in vivo pain models, NP-1815-PX sodium is typically dissolved in saline or a suitable vehicle and administered via intrathecal injection (doses ranging from 10-100 ug/mouse) in mouse models of neuropathic pain (e.g., partial sciatic nerve ligation or spinal nerve ligation). Alternatively, intraperitoneal administration (1-10 mg/kg) may be used. Allodynia and hyperalgesia are measured using von Frey filaments and Hargreaves test, respectively, at various time points post-administration (0-6 hours).
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| ADME/Pharmacokinetics |
Detailed PK data for NP-1815-PX sodium are limited in publicly available literature. As a sodium salt, the compound has improved aqueous solubility. In rodent studies, NP-1815-PX sodium is typically administered via intrathecal or intraperitoneal routes. Researchers should refer to primary research articles or conduct pilot PK studies to determine parameters such as half-life, bioavailability, and brain penetration for their specific model.
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| Toxicity/Toxicokinetics |
Published toxicology data for NP-1815-PX sodium are limited. In cell-based assays at concentrations up to 10 uM, no significant cytotoxicity has been reported. In animal studies, intrathecal administration at effective analgesic doses does not affect motor function or acute nociceptive pain, suggesting a favorable safety profile in the central nervous system. Comprehensive toxicology studies have not been publicly released.
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| References |
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| Additional Infomation |
NP-1815-PX sodium is a research tool and is not approved for clinical use. It has no ongoing clinical trials. The compound is used to investigate the role of P2X4 receptors in chronic pain, neuroinflammation, and respiratory conditions. It is selective for P2X4R over other P2X subtypes, making it a valuable tool for dissecting P2X4-mediated signaling. The compound should be stored at -20degC, protected from moisture and light.
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| Molecular Formula |
C21H13N4NAO3S
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|---|---|
| Molecular Weight |
424.407693624496
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| Exact Mass |
424.06
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| CAS # |
1239578-80-3
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| Related CAS # |
NP-1815-PX;1239578-79-0
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| PubChem CID |
154731051
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
30
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| Complexity |
748
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C(=O)NC2=C(C=CC3=CC=CC=C32)N(C1=O)C4=CC=CC(=C4)C5=NOC(=S)[N-]5.[Na+]
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| InChi Key |
MIBCQKIVVIBTLQ-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C21H14N4O3S.Na/c26-17-11-18(27)25(14-6-3-5-13(10-14)20-23-21(29)28-24-20)16-9-8-12-4-1-2-7-15(12)19(16)22-17;/h1-10H,11H2,(H2,22,23,24,26,29);/q;+1/p-1
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| Chemical Name |
sodium;5-[3-(5-sulfanylidene-1-oxa-2-aza-4-azanidacyclopent-2-en-3-yl)phenyl]-1H-benzo[g][1,5]benzodiazepine-2,4-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2356 mL | 1.1781 mL | 2.3562 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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