| 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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| Other Sizes |
Purity: ≥98%
| Targets |
The primary target of CDPPB is the metabotropic glutamate receptor 5 (mGluR5). It acts as a positive allosteric modulator (PAM), binding to an allosteric site on the receptor and enhancing the response to glutamate. This increases mGluR5 activity, which is involved in learning, memory, synaptic plasticity, and the regulation of neurotransmission.
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| ln Vitro |
In vitro, CDPPB has been shown to potentiate mGluR5-mediated signaling in cell-based assays. It enhances glutamate-induced calcium mobilization and other downstream signaling events. The compound's selectivity for mGluR5 over other mGluR subtypes has been confirmed in receptor binding and functional assays.
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| ln Vivo |
In vivo, CDPPB has been shown to have antipsychotic and anxiolytic effects in animal models. It reverses behavioral deficits in models of schizophrenia and reduces anxiety-like behavior in rodents. The compound is orally active and has been evaluated in preclinical studies for its potential therapeutic applications in neuropsychiatric disorders.
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| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for CDPPB involve studying its binding to the mGluR5 receptor. Radioligand binding assays are performed using membrane preparations from cells expressing mGluR5. The compound is incubated with a radiolabeled ligand, and the displacement of the ligand is measured to determine the affinity. Functional assays, such as calcium mobilization assays, are used to assess its PAM activity.
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| Cell Assay |
In vitro cell-based assays for CDPPB are performed using cells that express mGluR5. Cells are loaded with a calcium-sensitive fluorescent dye and treated with the compound in the presence of a submaximal concentration of glutamate. The potentiation of the calcium response is measured as a functional readout of PAM activity. The compound's effects on cell signaling and gene expression are also assessed.
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| Animal Protocol |
In vivo animal experiments for CDPPB are conducted using rodent models of schizophrenia and anxiety. The compound is administered orally or intraperitoneally, and its effects on behavior, such as prepulse inhibition, social interaction, and anxiety-like behavior, are assessed. The compound's effects on brain mGluR5 activity and neurotransmitter levels are also measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of CDPPB indicate that it is orally active. The compound has a molecular weight of 361.41 and a molecular formula of C21H19N3O3. It is a solid at room temperature. Specific PK parameters, such as half-life and bioavailability, are determined in preclinical studies via LC-MS/MS analysis of plasma samples. The compound is metabolized in the liver and excreted renally.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for CDPPB are characteristic of a research compound. As an mGluR5 PAM, its safety profile is an important consideration. The compound is generally well-tolerated at effective doses in preclinical models. Common side effects may include headache, dizziness, and gastrointestinal disturbances. Long-term safety data are being evaluated in ongoing studies.
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| References |
Doria JG, de Souza JM, Andrade JN, Rodrigues HA, Guimaraes IM, Carvalho TG, Guatimosim C, Dobransky T, Ribeiro FM. The mGluR5 positive allosteric modulator, CDPPB, ameliorates pathology and phenotypic signs of a mouse model of Huntington's disease. Neurobiol Dis. 2015 Jan;73:163-73.
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| Additional Infomation |
Other information: CDPPB is a research compound used to study the role of mGluR5 in neuropsychiatric disorders. It is a positive allosteric modulator of mGluR5. The compound is available from chemical suppliers for preclinical research purposes. Its CAS number is 781652-57-1.
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| Molecular Formula |
C23H16N4O
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| Molecular Weight |
364.39934
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| Exact Mass |
364.132
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| CAS # |
781652-57-1
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| Related CAS # |
781652-57-1;
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| PubChem CID |
11245456
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| Appearance |
White to off-white solid powder
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| Density |
1.203g/cm3
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| Boiling Point |
523.277ºC at 760 mmHg
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| Flash Point |
270.268ºC
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| Index of Refraction |
1.655
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| LogP |
4.736
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
572
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BKUIZWILNWHFHD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H16N4O/c24-16-17-8-7-11-19(14-17)23(28)25-22-15-21(18-9-3-1-4-10-18)26-27(22)20-12-5-2-6-13-20/h1-15H,(H,25,28)
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| Chemical Name |
3-cyano-N-(2,5-diphenylpyrazol-3-yl)benzamide
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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 : ~100 mg/mL (~274.42 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (13.72 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 50.0 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 | 2.7442 mL | 13.7212 mL | 27.4424 mL | |
| 5 mM | 0.5488 mL | 2.7442 mL | 5.4885 mL | |
| 10 mM | 0.2744 mL | 1.3721 mL | 2.7442 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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