| 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 |
| Targets |
rat mGluR5 9 nM (EC50) rat mGluR1 557 nM (EC50) rat mGluR2 1.5 μM (EC50) hmGluR4 154 nM (EC50) rat mGluR5 224 nM (Ki)
mGluR5 (metabotropic glutamate receptor 5). |
|---|---|
| ln Vitro |
VU-29 potentiates the rat mGlu5 receptor with an EC50 of 9 nM and binds with an apparent Ki of 244 nM. It is selective for mGluR5 over other mGluR subtypes, with EC50 values of 557 nM for rmGluR1, 1.5 μM for rmGluR2, and 154 nM for hmGluR4. This high potency and selectivity make it a preferred tool for studying mGlu5 receptor function.
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| ln Vivo |
In rat hippocampal slices, VU-29 (500 nM) amplifies the effects of DHPG on phosphoinositide (PI)-induced hydrolysis. In the rat hippocampus CA1 area, VU-29 enhances threshold TBS-induced long term potentiation (LTP). In rat hippocampal region CA1, VU-29 (1 µM) enhances chemically induced mGluR-long term depression (LTD). VU-29 (1 µM) enhances NMDA receptor-independent LTD caused by stimuli[1].
In rat hippocampal slices, VU-29 (500 nM) potentiates DHPG-induced increases in phosphoinositide (PI) hydrolysis. It also potentiates threshold TBS-induced long-term potentiation (LTP) in the rat hippocampal CA1 region. In vivo, VU-29 has been shown to prevent ethanol-induced impairments in spatial memory retrieval and to normalize ethanol withdrawal-induced changes in mGlu5 and mGlu2 receptor protein expression. |
| Enzyme Assay |
In vitro receptor binding assays are performed using membranes from cells expressing rat mGlu5 receptors. Radioligand binding studies with [3H]-MPEP or similar compounds are conducted to determine the allosteric binding affinity (Ki) of VU-29. The compound's ability to displace the radioligand from the allosteric site is measured to establish its binding characteristics.
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| Cell Assay |
Cells expressing recombinant mGlu5 receptors are treated with a sub-maximal concentration of glutamate (e.g., EC20) in the presence of varying concentrations of VU-29. The potentiation of receptor activity is measured by assessing downstream signaling, such as intracellular calcium mobilization or PI hydrolysis. The EC50 for the potentiating effect is determined from the concentration-response curve.
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| Animal Protocol |
In vivo studies are conducted in rodent models to evaluate the cognitive and behavioral effects of mGlu5 PAMs. VU-29 is typically administered systemically (e.g., via i.p. or oral gavage) to assess its effects on learning and memory tasks, such as the Morris water maze or novel object recognition. Its impact on drug-induced behaviors, such as ethanol-induced memory impairment, can also be evaluated.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for VU-29. As a research compound, its PK properties would be characterized in standard rodent studies following intravenous and oral administration to determine parameters like bioavailability, half-life, and brain penetration. Such data are essential for designing appropriate in vivo dosing regimens.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for VU-29. As a PAM, its toxicity profile is expected to be related to its mechanism of action, potentially enhancing glutamatergic signaling. Overstimulation of mGlu5 receptors could lead to excitotoxicity or other CNS-related side effects. Standard safety assessments would be required for any therapeutic development.
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| References |
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| Additional Infomation |
mGluR5 is a positive allosteric modifier; its structure is described in the first reference.
VU-29 is a highly potent and selective mGlu5 PAM that is widely used in preclinical research. Its ability to enhance mGlu5 function has made it a key tool for studying the receptor's role in synaptic plasticity, learning, and memory. It is not approved for clinical use and is strictly for research purposes. The compound is also used to investigate the therapeutic potential of mGlu5 PAMs in various CNS disorders. |
| Molecular Formula |
C22H16N4O3
|
|---|---|
| Molecular Weight |
384.39
|
| Exact Mass |
384.122
|
| CAS # |
890764-36-0
|
| PubChem CID |
11610682
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
5.296
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
29
|
| Complexity |
561
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC=C(C=C1)C2=NN(C(=C2)NC(=O)C3=CC=C(C=C3)[N+](=O)[O-])C4=CC=CC=C4
|
| InChi Key |
KIALCSMRIHRFPL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H16N4O3/c27-22(17-11-13-19(14-12-17)26(28)29)23-21-15-20(16-7-3-1-4-8-16)24-25(21)18-9-5-2-6-10-18/h1-15H,(H,23,27)
|
| Chemical Name |
N-(2,5-diphenylpyrazol-3-yl)-4-nitrobenzamide
|
| 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 (130.08 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (13.01 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6015 mL | 13.0076 mL | 26.0152 mL | |
| 5 mM | 0.5203 mL | 2.6015 mL | 5.2030 mL | |
| 10 mM | 0.2602 mL | 1.3008 mL | 2.6015 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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