NP10679
Based on 1 Customer Validation
NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.40%
- Fòrmula: C23H26F3N3O3
- Peso molecular:449.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Ver todos los productos específicos de isoformas iGluR
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Actividad biológica
Descripciòn
IC50 & Target
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H1 Receptor 0.073 μM (IC50) |
H1 Receptor 0.04 μM (Ki) |
Alpha-1A adrenergic receptor 0.154 μM (IC50) |
Alpha-1A adrenergic receptor 0.603 μM (Ki) |
Alpha-1B adrenergic receptor 1.92 μM (Ki) |
Alpha-1D adrenergic receptor 0.495 μM (Ki) |
Alpha-2C adrenergic receptor 3.09 μM (Ki) |
In Vitro
NP10679 (1-1000 nM) shows pH-dependently effects to GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively[2]. NP10679 shows functional inhibition to 5-HT2A, α adrenergic receptor-1A (α1A), H1-histamine receptor (H1) and hERG channel with IC50 values of 1.71, 0.154, 0.073 and 0.617 μM, respectively[2]. NP10679 shows Ki values of 2.29, 0.638, 1.92, 0.603, 1.92, 0.495, 3.09, 0.040 and 0.135 for 5-HT1D, 5-HT2A, 5-HT2B, α1A, α1B, α1D, α2C, H1 and serotonin transporter SERT[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 middle cerebral artery occlusion (MCAo) model of transient ischemia mice[2]
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Dosage:2, 5 and 10 mg/kg
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Administration:Intraperitoneal injection; 2, 5 and 10 mg/kg, 15 minutes prior to transient ischemia
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Result:Dose-dependently reduced infarct volumes with an ED50 of 1 mg/kg.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Appearance Solid
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Peso molecular 449.47
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Fòrmula C23H26F3N3O3
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Color White to light yellow
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SMILES
O=C(N1)CCC2=C1C=CC(OC[C@H](O)CN(CC3)CCN3C4=CC=C(C(F)(F)F)C=C4)=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (222.48 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. 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. 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.56 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.56 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zaczek R, et al. Phase 1 Clinical Results for NP10679, a pH-sensitive GluN2B-selective N-methyl-d-aspartate Receptor Inhibitor. Clin Pharmacol Drug Dev. 2023 Jan 15. [Content Brief]
[2]. Myers SJ, et al. A Glutamate N-Methyl-d-Aspartate (NMDA) Receptor Subunit 2B-Selective Inhibitor of NMDA Receptor Function with Enhanced Potency at Acidic pH and Oral Bioavailability for Clinical Use. J Pharmacol Exp Ther. 2021 Oct;379(1):41-52. [Content Brief]
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. 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 |
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| DMSO | 1 mM | 2.2248 mL | 11.1242 mL | 22.2484 mL | 55.6211 mL |
| 5 mM | 0.4450 mL | 2.2248 mL | 4.4497 mL | 11.1242 mL | |
| 10 mM | 0.2225 mL | 1.1124 mL | 2.2248 mL | 5.5621 mL | |
| 15 mM | 0.1483 mL | 0.7416 mL | 1.4832 mL | 3.7081 mL | |
| 20 mM | 0.1112 mL | 0.5562 mL | 1.1124 mL | 2.7811 mL | |
| 25 mM | 0.0890 mL | 0.4450 mL | 0.8899 mL | 2.2248 mL | |
| 30 mM | 0.0742 mL | 0.3708 mL | 0.7416 mL | 1.8540 mL | |
| 40 mM | 0.0556 mL | 0.2781 mL | 0.5562 mL | 1.3905 mL | |
| 50 mM | 0.0445 mL | 0.2225 mL | 0.4450 mL | 1.1124 mL | |
| 60 mM | 0.0371 mL | 0.1854 mL | 0.3708 mL | 0.9270 mL | |
| 80 mM | 0.0278 mL | 0.1391 mL | 0.2781 mL | 0.6953 mL | |
| 100 mM | 0.0222 mL | 0.1112 mL | 0.2225 mL | 0.5562 mL |
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