Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
Submit ReviewVU 0483605
Description: Positive allosteric modulator of mGlu1 receptors
Chemical Name: 3-Chloro-N-[3-chloro-4-(4-chloro-1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)phenyl]-2-pyridinecarboxamide
Purity: ≥98% (HPLC)
Biological Activity
Positive allosteric modulator at mGlu1 (EC50 values are 356 and 390 nM for rat and human receptors, respectively). Exhibits >25-fold selectivity for mGlu1 over mGlu4. Potentiates the decreased glutamate-induced calcium response in mGlu1 mutant cell models of schizophrenia.
Technical Data
| M. Wt | 446.67 |
| Formula | C20H10Cl3N3O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1623101-11-0 |
| PubChem ID | 91885483 |
| InChI Key | HJQXPBKPTGWZCF-UHFFFAOYSA-N |
| Smiles | ClC1=C2C(C(N(C3=CC=C(NC(C4=C(Cl)C=CC=N4)=O)C=C3Cl)C2=O)=O)=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 22.33 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 446.67. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.48 mL | 22.39 mL | 44.78 mL |
| 2.5 mM | 0.9 mL | 4.48 mL | 8.96 mL |
| 5 mM | 0.45 mL | 2.24 mL | 4.48 mL |
| 25 mM | 0.09 mL | 0.45 mL | 0.9 mL |
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
Product Datasheets
References
References are publications that support the biological activity of the product.
Cho et al (2014) Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics. ACS Chem.Biol. 9 2334 PMID: 25137254
If you know of a relevant reference for VU 0483605, please let us know.
View Related Products by Target
View Related Products by Product Action
View all Glutamate (Metabotropic) Group I Receptor Modulators
Keywords: VU 0483605, VU 0483605 supplier, VU0483605, positive, allosteric, modulators, PAMs, mglu1, metabotropic, glutamate, receptors, schizophrenia, Glutamate, (Metabotropic), Group, I, Receptors, 5377, Tocris Bioscience
1 Citation for VU 0483605
Citations are publications that use Tocris products. Selected citations for VU 0483605 include:
Hellyer et al (2018) "Selective" Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu5 Allosteric Ligands. Mol.Pharmacol. 93 504 PMID: 29514854
Do you know of a great paper that uses VU 0483605 from Tocris? Please let us know.
Reviews for VU 0483605
There are currently no reviews for this product. Be the first to review VU 0483605 and earn rewards!
Have you used VU 0483605?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
GPCR Product Listing
A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:
- Rhodopsin-like Receptors
- Glutamate Receptors
- Frizzled Receptors
- GPCR Signaling
Pain Research Product GuideUpdated
A collection of over 280 products for pain research, the guide includes research tools for the study of:
- Nociception
- Ion Channels
- G-Protein-Coupled Receptors
- Intracellular Signaling
Metabotropic Glutamate Receptors Scientific Review
Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.
Addiction Poster
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Epilepsy Poster
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Huntington's Disease Poster
Huntington's disease (HD) is a monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the MSN intracellular signaling pathways implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Pain Poster
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Parkinson's Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.