VU 0361737 (Synonyms: ML-128) |
| Catalog No.GC13962 |
MGlu4 receptor allosteric modulator
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1161205-04-4
Sample solution is provided at 25 µL, 10mM.
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VU0361737 is a selective, positive allosteric modulator and brain-permeable for mGLuR4 (mGlu4 receptor), (EC₅₀ = 240 and 110 nM for human and rat receptors respectively), >50 fold selectivity over other mGluR subtypes. Inactive at mGluR-1, mGluR-2, mGluR-3, mGluR-6 and mGluR-7 receptors and showed weak activity at mGluR-5 and mGluR-8 receptors. [1]
The mGluR (metabotropic glutamate receptor) is a group of G-protein coupled receptors and is active through an indirect metabotropic process. mGLuR4 are invoinved in Parkinson as it decrease GABAerigic transmission at inhibitory striato-pallidal synapse with the basal ganglia.[1][2]
Following the administration of VU0361737 into rat intraperitoneally (10mg/kg), the amount of compound present in brain and plasma was determined at 0.5, 1 and 8 hours. It showed a short half-life (T1/2 20 minutes) and a pronounced brain exposure (brain: plasma ratio = 4.1) [1]
References:
[1] Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J Med Chem. 2009 Jul 23;52(14):4115-8.
[2] Engers DW, Field JR, Le U, Zhou Y, Bolinger JD, Zamorano R, Blobaum AL, Jones CK, Jadhav S, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. J Med Chem. 2011 Feb 24;54(4):1106-10.
| Cas No. | 1161205-04-4 | SDF | |
| Synonyms | ML-128 | ||
| Chemical Name | N-(4-chloro-3-methoxyphenyl)pyridine-2-carboxamide | ||
| Canonical SMILES | COC1=C(C=CC(=C1)NC(=O)C2=CC=CC=N2)Cl | ||
| Formula | C13H11ClN2O2 | M.Wt | 262.69 |
| Solubility | DMF: 50 mg/ml,DMSO: 50 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml,Ethanol: 10 mg/ml | 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. |
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| 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 | 3.8068 mL | 19.0338 mL | 38.0677 mL |
| 5 mM | 0.7614 mL | 3.8068 mL | 7.6135 mL |
| 10 mM | 0.3807 mL | 1.9034 mL | 3.8068 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)
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