VU0483605 |
| カタログ番号GC11667 |
VU0483605 は、脳に浸透する強力な mGlu1 受容体ポジティブ アロステリック モジュレーター (PAM) です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1623101-11-0
Sample solution is provided at 25 µL, 10mM.
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VU0483605 is a selective positive allosteric modulator (PAM) of mGluR1 [1].
The metabotropic glutamate receptors (mGluRs), members of G-protein-coupled receptors, have been involved in a variety of functions in the central and peripheral nervous systems, such as learning, memory, anxiety, and the perception of pain. The mGluRs exist in pre- and postsynaptic neurons in synapses of the hippocampus, cerebellum, the cerebral cortex, as well as other parts of the brain and in peripheral tissues. Mice deficient in mGluR1 showed severe motor coordination and spatial learning deficient [2].
VU0483605 is a selective positive allosteric modulator (PAM) of mGluR1. VU0483605 displayed EC50 values of 0.39 and 0.36 μM at human and rat mGluR1 receptors, respectively. VU0483605 showed no activity against mGlu4 PAM with the EC50 of >10 μM. VU0483605 potentiated the response to glutamate in cells stably expressing mGlu1 and partially restored the reduction in glutamate-mediated calcium signaling in a mutant cell model of schizophrenia [1].
References:
[1] Cho H P, Garcia-Barrantes P M, Brogan J T, et al. Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics[J]. ACS chemical biology, 2014, 9(10): 2334-2346.
[2] Conquet F, Bashir Z I, Davies C H, et al. Motor deficit and impairment of synaptic plasticity in mice lacking mGluR1[J]. Nature, 1994, 372(6503): 237.
| Cas No. | 1623101-11-0 | SDF | |
| Chemical Name | 3-chloro-N-[3-chloro-4-(4-chloro-1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)phenyl]-2-pyridinecarboxamide | ||
| Canonical SMILES | O=C1N(C2=CC=C(NC(C3=C(Cl)C=CC=N3)=O)C=C2Cl)C(C4=CC=CC(Cl)=C41)=O | ||
| Formula | C20H10Cl3N3O3 | M.Wt | 446.7 |
| 溶解度 | ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2386 mL | 11.1932 mL | 22.3864 mL |
| 5 mM | 447.7 μL | 2.2386 mL | 4.4773 mL |
| 10 mM | 223.9 μL | 1.1193 mL | 2.2386 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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