NYX-2925
Based on 1 Customer Validation
NYX-2925 is an orally active NMDAR modulator. NYX-2925 restores levels of activated Src and Src phosphorylation sites on GluN2A and GluN2B in the mPFC. NYX-2925 shows no effect on CAMKII, and any addictive or sedative/ataxic side effects. NYX-2925 can be used for research of a variety of NMDA receptor-mediated central nervous system disorders.
For research use only. We do not sell to patients.
- Purity: 98.98%
- CAS No.: 2012536-16-0
- Formula: C14H23N3O4
- Molecular Weight:297.35
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All iGluR Isoforms
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Biological Activity
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NMDA Receptor |
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Animal Model:Sprague Dawley (adult male, 2-3 months old, chronic constriction injury of the sciatic nerve)[2]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Reversed CCI-induced mechanical hypersensitivity, with paw withdrawal thresholds increased from <5 g to SHAM levels 1 hour post-dose (F(5,60)=45.67, p=0.0012; F(2,41)=56.66, p<0.0001).
Restored CCI-induced decreases in phosphorylated Src (Tyr416) in mPFC whole cell lysates (p=0.0001) and synaptosomal fractions (p=0.0090) to SHAM levels.
Restored CCI-induced decreases in Src-mediated phosphorylation sites on GluN2A (Tyr1246: p=0.0003 in whole lysates, p=0.0228 in synaptosomes; Tyr1325: trend toward restoration in synaptosomes) and GluN2B (Tyr1472: p=0.0005 in whole lysates; Tyr1252: p=0.0002 in whole lysates, p=0.0414 in synaptosomes) to SHAM levels, with no effect on phosphorylated CAMKIIα (Thr286) or GluN2B (Ser1303) levels.
Showed no effect on paw withdrawal thresholds or phosphorylated Src levels in SHAM rats.
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Animal Model:Sprague-Dawley (male, 2-3-month old, 250-350 g, streptozotocin-induced diabetic neuropathy)[5]
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Dosage:0.1 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o. ; single dose
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Result:Significantly increased paw withdrawal threshold versus vehicle at 1 hour, 24 hours, and 1 week post single oral 10 mg/kg dosing; significantly increased paw withdrawal threshold at 1 hour and 1 week post single oral 3 mg/kg dosing; significantly increased paw withdrawal threshold at 1 hour post single oral 1 mg/kg dosing; showed no effect at any time point with single oral 0.1 mg/kg dosing.
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Animal Model:Sprague-Dawley (male, 2-3-month old, 250-350 g, formalin-induced persistent pain)[5]
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Dosage:0.1 mg/kg; 1 mg/kg; 10 mg/kg
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Administration:p.o. ; single dose
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Result:Significantly reduced average phase II pain responses from 18.24 (vehicle) to 8.17 with single oral 1 mg/kg dosing.
Significantly reduced average phase II pain responses from 18.24 (vehicle) to 5.70 with single oral 10 mg/kg dosing.
Showed no effect with single oral 0.1 mg/kg dosing.
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Animal Model:Sprague-Dawley (male, 2-3-month old, 250-350 g, tail flick test for acute nociceptive pain)[5]
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Dosage:0.1 mg/kg; 1 mg/kg; 10 mg/kg
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Administration:p.o. ; single dose
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Result:Showed no significant effect on tail flick latency versus vehicle, with values similar to baseline at all tested oral doses.
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Animal Model:Sprague-Dawley (male, 2- to 3-month-old, sleep deprivation model)[6]
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Dosage:0.1 mg/kg; 1 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Increased NREM sleep time and total sleep time during the lights-on phase in both non-sleep-deprived and sleep-deprived rats at 1 mg/kg, without affecting REM sleep.
Facilitated NREM sleep 24 hours post-dosing in sleep-deprived rats at 0.1, 1, and 10 mg/kg.
Showed persistent NREM sleep facilitation at 48 and 72 hours post-dosing in sleep-deprived rats at 10 mg/kg.
Increased sleep-bout duration, increased NREM to REM latency, decreased delta power in wake, and increased delta power in NREM and theta power in REM across 3 testing days at 10 mg/kg.
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Animal Model:Sprague-Dawley (male, sleep deprivation model)[6]
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Dosage:1 mg/kg
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Administration:p.o.; single dose;
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Result:Increased rates of hedonic 50-kHz USVs.
Increased rates of hedonic 50-kHz USVs and decreased rates of aversive 20-kHz USVs in response to unconditioned play.
Increased running speed to self-administer play.
Showed significant differences between NYX-2925 and sleep-deprived vehicle groups in all measured endpoints.
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Animal Model:Sprague-Dawley (male)[6]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Enhanced the amplitude of positive affect (50-kHz USVs) during the dark phase.
Suppressed negative affect (20-kHz USVs) across the 24-hour period.
Enhanced the amplitude of the locomotor activity rhythm by decreasing activity during the light phase.
Improved the accuracy of the light-dark transition for locomotor activity, reducing absolute error vs. lights-on time to 15.9 minutes (vs. vehicle 34.0 minutes).
Decreased fragmentation of diurnal behavior to 14.6% (vs. vehicle 34.0%).
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Animal Model:Sprague Dawley (male, 60 days old)[7]
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Dosage:1 mg/kg
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Administration:p.o.; single dose
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Result:Increased levels of GluN2B in PSD-95 co-immunoprecipitates of the rat prefrontal cortex 24 hours after dosing.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2012536-16-0
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Appearance Solid
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Molecular Weight 297.35
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Formula C14H23N3O4
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Color White to off-white
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SMILES
CC(C)C(N1[C@@]2(CCC1)C(N(C2)[C@H](C(N)=O)[C@H](O)C)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (336.30 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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)
Purity & Documentation
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Data Sheet (278 KB)
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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)
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Handling Instructions (2659 KB)
References
[1]. Zeng Y, et al. New advances in small molecule drugs targeting NMDA receptors. Acta pharmacologica Sinica. 2026 Jan;47(1):3-21. [Content Brief]
[2]. Morrison G, et al. The NMDAR modulator NYX-2925 alleviates neuropathic pain via a Src-dependent mechanism in the mPFC. Neurobiology of pain (Cambridge, Mass.). 2020;7:100039. [Content Brief]
[3]. Houck DR, et al. NYX-2925, A Novel N-methyl-D-aspartate Receptor Modulator: A First-in-Human, Randomized, Double-blind Study of Safety and Pharmacokinetics in Adults. Clinical and translational science. 2019 Mar;12(2):164-171. [Content Brief]
[4]. Burgdorf JS, et al. A translational EEG-based approach to assess modulation of long-lasting NMDAR-dependent synaptic plasticity. Psychopharmacology. 2019 Dec;236(12):3687-3693. [Content Brief]
[5]. Ghoreishi-Haack N, et al. NYX-2925 Is a Novel -Methyl-d-Aspartate Receptor Modulator that Induces Rapid and Long-Lasting Analgesia in Rat Models of Neuropathic Pain. The Journal of pharmacology and experimental therapeutics. 2018 Sep;366(3):485-497. [Content Brief]
[6]. Burgdorf JS, et al. NMDAR activation regulates the daily rhythms of sleep and mood. Sleep. 2019 Oct 09;42(10):zsz135. [Content Brief]
[7]. Bowers MS, et al. NYX-2925 induces metabotropic N-methyl-d-aspartate receptor (NMDAR) signaling that enhances synaptic NMDAR and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor. Journal of neurochemistry. 2020 Mar;152(5):523-541. [Content Brief]
[8]. Khan MA, et al. NYX-2925 Is a Novel NMDA Receptor-Specific Spirocyclic-β-Lactam That Modulates Synaptic Plasticity Processes Associated with Learning and Memory. The international journal of neuropsychopharmacology. 2018 Mar 01;21(3):242-254. [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 (protect from light, stored under nitrogen). 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 | 3.3630 mL | 16.8152 mL | 33.6304 mL | 84.0760 mL |
| 5 mM | 0.6726 mL | 3.3630 mL | 6.7261 mL | 16.8152 mL | |
| 10 mM | 0.3363 mL | 1.6815 mL | 3.3630 mL | 8.4076 mL | |
| 15 mM | 0.2242 mL | 1.1210 mL | 2.2420 mL | 5.6051 mL | |
| 20 mM | 0.1682 mL | 0.8408 mL | 1.6815 mL | 4.2038 mL | |
| 25 mM | 0.1345 mL | 0.6726 mL | 1.3452 mL | 3.3630 mL | |
| 30 mM | 0.1121 mL | 0.5605 mL | 1.1210 mL | 2.8025 mL | |
| 40 mM | 0.0841 mL | 0.4204 mL | 0.8408 mL | 2.1019 mL | |
| 50 mM | 0.0673 mL | 0.3363 mL | 0.6726 mL | 1.6815 mL | |
| 60 mM | 0.0561 mL | 0.2803 mL | 0.5605 mL | 1.4013 mL | |
| 80 mM | 0.0420 mL | 0.2102 mL | 0.4204 mL | 1.0510 mL | |
| 100 mM | 0.0336 mL | 0.1682 mL | 0.3363 mL | 0.8408 mL |
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