| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
CIQ selectively potentiates NMDA receptors containing the GluN2C or GluN2D subunits. It acts as a positive allosteric modulator, binding to a site distinct from the glutamate and glycine binding sites. This enhances the channel opening frequency and efficiency, leading to increased NMDA receptor responses. The GluN2C and GluN2D subunits are predominantly expressed in the cerebellum, thalamus, and brainstem, making CIQ a valuable tool for studying the function of these receptor subtypes.
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| ln Vitro |
In vitro, CIQ potentiates NMDA receptor-mediated currents in cells expressing GluN2C- or GluN2D-containing receptors with EC50 values of 2.7 μM and 2.8 μM, respectively. It enhances receptor responses approximately two-fold by increasing channel opening frequency for glutamate or glycine. CIQ does not affect the EC50 values for glutamate or glycine, indicating that it acts as a positive allosteric modulator rather than an agonist. It has no effect at GluN2A, GluN2B, or non-NMDA glutamate receptors.
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| ln Vivo |
CIQ reverses MK-801-induced impairment in prepulse inhibition and working memory in the Y-maze test in mice. This suggests that potentiating GluN2C/GluN2D-containing NMDA receptors may have therapeutic benefits for cognitive symptoms and positive symptoms in schizophrenia. CIQ may also enhance dopamine release in Parkinson's disease models. These in vivo effects highlight the potential of GluN2C/D-selective positive allosteric modulators for treating neuropsychiatric disorders.
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| Enzyme Assay |
In vitro assays for CIQ typically involve electrophysiological recordings from cells expressing recombinant NMDA receptors. HEK293 cells or Xenopus oocytes are transfected with NMDA receptor subunit combinations (e.g., GluN1 + GluN2C or GluN1 + GluN2D). Two-electrode voltage-clamp or patch-clamp techniques are used to measure receptor currents in response to glutamate and glycine application in the presence and absence of CIQ. Potentiation is quantified as the percentage increase in current amplitude, and EC50 values are determined from concentration-response curves.
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| Cell Assay |
Cellular assays for CIQ are performed using cell lines expressing recombinant NMDA receptors. Cells are treated with CIQ at varying concentrations (typically 0.1-100 μM) for a defined period. Receptor function may be assessed by calcium imaging using fluorescent indicators such as Fura-2 or Fluo-4, or by measuring intracellular calcium levels with a plate reader. These assays provide a higher-throughput alternative to electrophysiology for assessing the modulatory effects of CIQ on NMDA receptor function.
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| Animal Protocol |
In vivo studies with CIQ are conducted in mouse models of schizophrenia and other neuropsychiatric disorders. MK-801, an NMDA receptor antagonist, is administered to induce schizophrenia-like behaviors, including prepulse inhibition deficits and working memory impairment. CIQ is administered prior to or concurrently with MK-801, and behavioral tests are performed to assess the reversal of these deficits. Doses and routes of administration are determined based on the compound's pharmacokinetic properties.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for CIQ are limited, as it is primarily a research compound. Its molecular weight is 467.94 g/mol, and it is soluble in DMSO but not in water. The compound's lipophilic nature suggests it can cross the blood-brain barrier, which is essential for its central nervous system activity. For in vivo studies, CIQ is typically formulated in suitable vehicles for oral or intraperitoneal administration. Its half-life and metabolic profile have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for CIQ are limited, as it is a research compound not intended for clinical use. In preclinical studies, no significant adverse effects have been reported at the doses used for behavioral experiments. Its selectivity for GluN2C/GluN2D-containing NMDA receptors minimizes off-target effects at other glutamate receptor subtypes. However, the compound should be handled with standard laboratory safety precautions.
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| References |
Kratz AL, Chadd E, Jensen MP, Kehn M, Kroll T. An examination of the psychometric properties of the community integration questionnaire (CIQ) in spinal cord injury. J Spinal Cord Med. 2014 Jan 3. [Epub ahead of print] PubMed PMID: 24621050.
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| Additional Infomation |
CIQ is a research compound used as a pharmacological tool to study the function of GluN2C/GluN2D-containing NMDA receptors. It has been used to investigate the role of these receptor subtypes in synaptic plasticity, learning, memory, and neuropsychiatric disorders. The facilitation of GluN2C/GluN2D-containing receptors may serve as an important therapeutic strategy for treating positive and cognitive symptoms in schizophrenia. CIQ is not approved for clinical use and is intended for laboratory research only.
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| Molecular Formula |
C26H26NO5CL
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|---|---|
| Molecular Weight |
467.94134
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| Exact Mass |
467.149
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| CAS # |
486427-17-2
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| Related CAS # |
486427-17-2;
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| PubChem CID |
4231127
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
635.8±55.0 °C at 760 mmHg
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| Flash Point |
338.3±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.590
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| LogP |
4.56
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
628
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VYMILMYEENZHAR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H26ClNO5/c1-30-20-7-9-21(10-8-20)33-16-23-22-15-25(32-3)24(31-2)14-17(22)11-12-28(23)26(29)18-5-4-6-19(27)13-18/h4-10,13-15,23H,11-12,16H2,1-3H3
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| Chemical Name |
(3-chlorophenyl)-[6,7-dimethoxy-1-[(4-methoxyphenoxy)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]methanone
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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 |
| 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 : ≥ 50 mg/mL (~106.85 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1370 mL | 10.6851 mL | 21.3703 mL | |
| 5 mM | 0.4274 mL | 2.1370 mL | 4.2741 mL | |
| 10 mM | 0.2137 mL | 1.0685 mL | 2.1370 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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