Product nameVU0155041 sodium salt, PAM for mGluR4
DescriptionPAM for mGluR4; water soluble
Biological descriptionPositive allosteric selective modulator at mGluR4 (EC50 values are 798 and 693 nM at human and rat mGluR4 receptors, respectively). It has advantages over PHCCC (ab120043) as it is water soluble and more potent. Shows limited blood-brain barrier permeability. Active in behavioural models of Parkinson's disease following icv injection.
Also available in simple stock solutions (ab146686) - add 1 ml of water to get an exact, ready-to-use concentration.
Chemical namecis-2-(3,5-Dichlorophenylcarbamoyl)cyclohexanecarboxylic acid sodium salt
Storage instructionsStore at Room Temperature. The product can be stored for up to 12 months.
Solubility overviewSoluble in water to 100 mM
This product is supplied in one (or more) pack size which is freeze dried. Therefore the contents may not be readily visible, as they can coat the bottom or walls of the vial. Please see our FAQs and information page for more details on handling.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Our Abpromise guarantee covers the use of ab120248 in the following tested applications.
The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.
|Functional Studies||Use at an assay dependent concentration.|
SKNSH cells were incubated at 37°C for 30 minutes with vehicle control (0 μM) and different concentrations of VU0155041 sodium salt (ab120248). Increased expression of Gli1 (ab49314) in SKNSH cells correlates with an decrease in VU0155041 sodium salt concentration, as described in literature.
Whole cell lysates were prepared with RIPA buffer (containing protease inhibitors and sodium orthovanadate), 30 μg of each were loaded on the gel and the WB was run under reducing conditions. After transfer the membrane was blocked for an hour using 5% BSA before being incubated with ab49314 at 2.5 μg/ml and ab8227 at 1 μg/ml overnight at 4°C. Antibody binding was detected using an anti- rabbit antibody conjugated to HRP (ab97051) at 1/10000 and visualised using ECL development solution.
This product has been referenced in:
- Williams R et al. Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4). Bioorg Med Chem Lett 19:4967-70 (2009). Read more (PubMed: 19640716) »
- Niswender CM et al. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol 74:1345-58 (2008). Read more (PubMed: 18664603) »