| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
DCB targets metabotropic glutamate receptor 5 (mGluR5), a G protein-coupled receptor that plays a critical role in synaptic transmission, plasticity, and neuronal excitability. mGluR5 is involved in various neurological and psychiatric disorders, including anxiety, depression, and addiction. As a neutral allosteric modulator, DCB binds to an allosteric site on mGluR5 and modulates the receptor's activity without directly activating or inhibiting it. It blocks the modulation of mGlu5 by other allosteric modulators without affecting agonist-stimulated mGlu5 responses.
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| ln Vitro |
In vitro, DCB acts as a neutral allosteric modulator of mGluR5. It inhibits the modulation of mGlu5 by other allosteric modulators without affecting agonist-stimulated mGlu5 responses. Its activity is concentration-dependent, with effective concentrations typically in the micromolar range. In cell-based assays, DCB modulates mGluR5-mediated signaling, as measured by calcium mobilization or IP3 accumulation. Its neutral modulatory effect makes it a valuable tool for studying mGluR5 function and allosteric modulation.
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| ln Vivo |
In vivo, DCB has been used in neuroscience research to study glutamatergic signaling and receptor modulation. Its ability to modulate mGluR5 activity may have implications for neurological and psychiatric disorders. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying mGluR5 function and allosteric modulation.
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| Enzyme Assay |
The in vitro mGluR5 modulation assay for DCB typically uses cells expressing recombinant mGluR5 (e.g., HEK293 cells) and measures calcium mobilization using a fluorescent calcium indicator such as Fluo-4. Cells are seeded in 96-well plates and treated with varying concentrations of the test compound (typically 0.1 to 100 µM) in the presence or absence of a mGluR5 agonist or positive allosteric modulator. Calcium flux is measured using a fluorescence plate reader. IC50 values for inhibition of other modulators are calculated from dose-response curves. Positive controls (e.g., known mGluR5 modulators) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, cells expressing mGluR5 are treated with DCB at concentrations ranging from 0.1 to 100 µM for 1-24 hours. Calcium mobilization is measured using fluorescent calcium indicators. Inositol phosphate accumulation is measured using radiolabeled assays. Cell viability is assessed using MTT or CellTiter-Glo assays. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo studies, DCB may be administered to rodents via intraperitoneal injection or oral gavage at doses ranging from 1 to 50 mg/kg. However, specific in vivo protocols for DCB are not well-documented in publicly available sources. The compound may be used in models of neurological or psychiatric disorders. All animal procedures should be conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of DCB have been partially characterized. The compound has a molecular weight of 277.15 and a molecular formula of C14H10Cl2N2. Following intraperitoneal or oral administration, the compound shows moderate absorption with a Tmax of 0.5-2 hours. Plasma half-life is estimated to be 2-4 hours. The compound distributes into tissues including brain, consistent with its central nervous system target. Metabolism is primarily hepatic, with CYP450-mediated oxidation as a major pathway. The compound is eliminated primarily via biliary and renal excretion. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of DCB are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
DCB (3,3'-Dichlorobenzaldazine) is a neutral allosteric modulator of mGluR5. It inhibits the modulation of mGlu5 by other allosteric modulators without affecting agonist-stimulated mGlu5 responses. It is used in neuroscience research to study glutamatergic signaling and receptor modulation. It is not approved for human use and is intended for research purposes only. It is available as a high-purity research reagent for laboratory use.
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| Molecular Formula |
C14H10N2CL2
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|---|---|
| Molecular Weight |
277.1486
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| Exact Mass |
276.022
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| CAS # |
6971-97-7
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| PubChem CID |
6861557
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.21g/cm3
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| Boiling Point |
387.794ºC at 760 mmHg
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| Flash Point |
188.331ºC
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| Index of Refraction |
1.59
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| LogP |
4.446
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
274
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC(=C1)Cl)/C=N/N=C/C2=CC(=CC=C2)Cl
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| InChi Key |
XMOVWXSCYLINBJ-BEQMOXJMSA-N
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| InChi Code |
InChI=1S/C14H10Cl2N2/c15-13-5-1-3-11(7-13)9-17-18-10-12-4-2-6-14(16)8-12/h1-10H/b17-9+,18-10+
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| Chemical Name |
(E)-1-(3-chlorophenyl)-N-[(E)-(3-chlorophenyl)methylideneamino]methanimine
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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 : ~25 mg/mL (~90.20 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (4.51 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 12.5 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 | 3.6082 mL | 18.0408 mL | 36.0815 mL | |
| 5 mM | 0.7216 mL | 3.6082 mL | 7.2163 mL | |
| 10 mM | 0.3608 mL | 1.8041 mL | 3.6082 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.
Link: https://clinicaltrials.gov/ct2/show/NCT01083030
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