DQP-1105
Based on 1 publication(s) in Google Scholar
DQP-1105 is a potent and selective NMDA receptor antagonist. DQP-1105 inhibits NMDA receptors containing GluN2C and GluN2D with IC50 values of 7.0 and 2.7 μM, respectively, and shows weaker inhibitory activity against receptors containing GluN2A or GluN2B. DQP-1105 exhibits higher affinity after the receptor binds glutamate, and inhibits high-frequency excitatory synaptic transmission by altering receptor gating kinetics or prolonging deactivation time. DQP-1105 can be used in research on epilepsy, depression, schizophrenia, and fragile X syndrome.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.05%
- CAS. Nr.: 380560-89-4
- Formel: C29H24BrN3O4
- Molecular Weight:558.42
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Speicherung:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) DQP-1105
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Biologische Aktivität
Beschreibung
IC50 & Target
[2]|
NR2C 7.0 μM (IC50) |
NR2D 2.7 μM (IC50) |
In Vitro
DQP-1105 (0.72-1.4 μM) inhibits GluN1/GluN2D receptors in a glutamate-dependent manner, with IC50 values of 1.4 μM at peak and 0.72 μM at steady-state[2].
DQP-1105-sensitive NR2C-containing NMDARs sustain the amplitude and period of PER2::LUC circadian oscillations in SCN slices[3].
DQP-1105 (20 µM) inhibits NAc core astrocytic NMDA receptor currents in WT mice by approximately 50% and reduces currents in saline-conditioned and conditioned mice, with greater inhibition in the conditioned group (47.84% current remaining) than in the saline group (61.96% current remaining)[6].
DQP-1105 inhibits GluN2D-containing NMDAR currents in mPFC PVIs from PV-Cre wild-type mice, reducing the response amplitude by about 40%, but does not inhibit NMDAR currents in PVIs from PV-GluN2D KO mice[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:primary cultured mouse cerebellar granule cells
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Concentration:20 µM, 40 µM
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Incubation Time:4 h
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Result:Significantly reduced neuronal nitric oxide synthase (nNOS) protein.
In Vivo
DQP-1105 (28 mg/kg; i.p.) reduces audiogenic seizure severity and death incidence in Fmr1 KO mice[8].
DQP-1105 (28 mg/kg; i.p.) increases audiogenic seizure incidence in wild-type littermate mice[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Fmr1 knockout (Fmr1 KO; juvenile male littermate mice, P20-22)[8]
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Dosage:28 mg/kg
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Administration:i.p.; single dose, 30 min prior to sound exposure
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Result:Reduced audiogenic seizure (AGS) scores and mortality rates.
Chemical Information
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CAS. Nr. 380560-89-4
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Appearance Solid
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Molecular Weight 558.42
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Formel C29H24BrN3O4
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Color White to off-white
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SMILES
O=C(CCC(N1N=C(CC1C2=CC=C(C=C2)Br)C3=C(C4=CC=CC=C4)C5=C(C=CC(C)=C5)NC3=O)=O)O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Sleep Med
Cerebellar GluN2C protects against sleep deprivation-induced cognitive impairment and motor incoordination. [Abstract]2025 Nov 8:137:108648. PMID: 41223665
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 10 mg/mL (17.91 mM; ultrasonic and warming and heat to 60°C; 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 (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 (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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 1 mg/mL (1.79 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Reinheit & Dokumentation
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Data Sheet (286 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)
Verweise
[2]. D'Erasmo MP, et al. Development of a Dihydroquinoline-Pyrazoline GluN2C/2D-Selective Negative Allosteric Modulator of the -Methyl-d-aspartate Receptor. ACS chemical neuroscience. 2023 Sep 06;14(17):3059-3076. [Content Brief]
[4]. Gao R, et al. NMDAR (2C) deletion in astrocytes relieved LPS-induced neuroinflammation and depression. International Immunopharmacology. 2024 May 10;132:111964. [Content Brief]
[5]. Zhou R, et al. Cerebellar GluN2C protects against sleep deprivation-induced cognitive impairment and motor incoordination. Sleep medicine. 2026 Jan;137:108648. [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 (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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7908 mL | 8.9538 mL | 17.9077 mL | 44.7692 mL |
| 5 mM | 0.3582 mL | 1.7908 mL | 3.5815 mL | 8.9538 mL | |
| 10 mM | 0.1791 mL | 0.8954 mL | 1.7908 mL | 4.4769 mL | |
| 15 mM | 0.1194 mL | 0.5969 mL | 1.1938 mL | 2.9846 mL |
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