NP10679 |
| Catalog No.GC71059 |
NP10679 는 선택적이고 pH 의존적인 GluN2B 아키 특이성 N-메틸-D-텐동아미노산(NMDA) 수용체 억제제로서 높은 경구 생체 이용도와 좋은 뇌 침투성을 가지고 있다.
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Cas No.: 2914889-88-4
Sample solution is provided at 25 µL, 10mM.
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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].
NP10679 (2, 5 and 10 mg/kg; i.p., prior to transient ischemia) reduces infarct volumes of transient ischemia mice[2].
References:
[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.
[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.
| Cas No. | 2914889-88-4 | SDF | |
| Formula | C23H26F3N3O3 | M.Wt | 449.47 |
| Solubility | 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) | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2248 mL | 11.1242 mL | 22.2484 mL |
| 5 mM | 0.445 mL | 2.2248 mL | 4.4497 mL |
| 10 mM | 0.2225 mL | 1.1124 mL | 2.2248 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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