| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
DQP-1105 targets the N-methyl-D-aspartate (NMDA) receptor, specifically the GluN2C and GluN2D subunits. It acts as a non-competitive antagonist and negative allosteric modulator, meaning it binds to a site distinct from the glutamate binding site to inhibit receptor function. It shows high selectivity for GluN2D (IC50 = 2.7 μM) and GluN2C (IC50 = 8.5 μM) over GluN2B (IC50 = 121 μM), GluK2 (IC50 = 153 μM), GluA1 (IC50 = 198 μM), and GluN2A (IC50 = 206 μM).
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|---|---|
| ln Vitro |
In vitro, DQP-1105 potently inhibits NMDA receptor function. Its IC50 values are 2.7 μM for GluN2D-containing receptors and 8.5 μM for GluN2C-containing receptors. It is significantly less potent against other receptor subtypes, demonstrating high selectivity. These characteristics make it a highly useful pharmacological tool for distinguishing GluN2C/D-mediated signaling from other glutamatergic pathways.
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| ln Vivo |
In vivo, DQP-1105 has potential applications in the treatment of neurological disabilities. As a selective antagonist of GluN2C/D receptors, it could help in understanding the role of these specific NMDA receptor subunits in various neurological and psychiatric conditions. However, detailed in vivo efficacy data is limited in standard research databases.
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| Enzyme Assay |
In vitro receptor binding and functional assays for DQP-1105 are typically performed using electrophysiology or calcium flux assays on cells expressing recombinant NMDA receptor subunits. The compound's potency and selectivity are determined by measuring its inhibition of agonist-induced currents or calcium influx.
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| Cell Assay |
For in vitro cellular assays, cell lines (e.g., HEK-293 cells) are transfected with specific NMDA receptor subunits (GluN1 + GluN2A, GluN2B, GluN2C, or GluN2D). Receptor function is measured using calcium-sensitive dyes or patch-clamp electrophysiology. DQP-1105 is applied at various concentrations, and the inhibition of receptor activity is recorded to calculate IC50 values.
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| Animal Protocol |
In vivo animal studies for DQP-1105 would involve administration to animal models of neurological or psychiatric disorders. Behavioral tests, electrophysiological recordings, and biochemical assays would be used to assess the compound's effects. However, standard in vivo protocols for this specific compound are not widely documented in public databases.
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| ADME/Pharmacokinetics |
DQP-1105 has a molecular weight of 558.42 g/mol and a molecular formula of C29H24BrN3O4. It is a solid compound typically stored at -20°C. It is soluble in DMSO, and stock solutions are often prepared for in vitro experiments.
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| Toxicity/Toxicokinetics |
DQP-1105 is a research chemical and is not intended for human therapeutic use. As with many research chemicals, standard safety precautions should be followed. Comprehensive toxicity data is not available in public databases. It is classified as a non-competitive NMDA receptor antagonist.
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| References | |
| Additional Infomation |
See also: Dqp-1105 (Notes moved to).
DQP-1105 is a potent and selective negative allosteric modulator of the GluN2C/D NMDA receptor. It is a highly valuable research tool for neuroscience, allowing for the specific study of GluN2C/D-containing NMDA receptors in the central nervous system. |
| Molecular Formula |
C29H24BRN3O4
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|---|---|
| Molecular Weight |
558.42256
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| Exact Mass |
557.095
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| CAS # |
380560-89-4
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| PubChem CID |
4235339
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| Appearance |
White to off-white solid powder
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| LogP |
5.594
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
37
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| Complexity |
964
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC2=C(C=C1)NC(=O)C(=C2C3=CC=CC=C3)C4=NN(C(C4)C5=CC=C(C=C5)Br)C(=O)CCC(=O)O
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| InChi Key |
ACUGSRUCGXYFTL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H24BrN3O4/c1-17-7-12-22-21(15-17)27(19-5-3-2-4-6-19)28(29(37)31-22)23-16-24(18-8-10-20(30)11-9-18)33(32-23)25(34)13-14-26(35)36/h2-12,15,24,28H,13-14,16H2,1H3,(H,35,36)
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| Chemical Name |
4-[3-(4-bromophenyl)-5-(6-methyl-2-oxo-4-phenyl-3H-quinolin-3-yl)-3,4-dihydropyrazol-2-yl]-4-oxobutanoic acid
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| Synonyms |
DQP1105 DQP 1105 DQP-1105.
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
DMSO : ~10 mg/mL (~17.91 mM)
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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 | 1.7908 mL | 8.9538 mL | 17.9077 mL | |
| 5 mM | 0.3582 mL | 1.7908 mL | 3.5815 mL | |
| 10 mM | 0.1791 mL | 0.8954 mL | 1.7908 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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