VU0361737
Based on 1 Customer Validation
VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.65%
- No. CAS: 1161205-04-4
- Fòrmula: C13H11ClN2O2
- Peso molecular:262.69
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Neurotransmitter Receptor Compound Library
HY-L062
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Neuroprotective Compound Library
HY-L070
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Anti-Parkinson's Disease Compound Library
HY-L085
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Neurodegenerative Disease-related Compound Library
HY-L086
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Targeted Diversity Library
HY-L099
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Heterocyclic Compound Library
HY-L138
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Highly Selective Activators Library
HY-L159
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Allosteric Modulators (AMs) Compound Library
HY-L170
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Lactylation Compound Library
HY-L249
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GPCR/G Protein Compound Library
HY-L006
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Neuronal Signaling Compound Library
HY-L013
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CNS-Penetrant Compound Library
HY-L028
Actividad biológica
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Human mGlu4 240 nM (EC50) |
Rat mGlu4 110 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
0.24 μM
Compound: 9b
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Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
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[PMID: 19469556] |
| CHO | IC50 |
12.8 nM
Compound: 1, ML128
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Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
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[PMID: 25330258] |
| CHO | IC50 |
5.1 nM
Compound: 2, ML-128
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Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
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[PMID: 26231155] |
| HEK293 | EC50 |
0.11 μM
Compound: 9b
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Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux
Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux
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[PMID: 19469556] |
VU0361737 displays weak activity at mGlu5 and mGlu8 receptors and inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors[1].
VU0361737 (1-10 μM) partially attenuates the Staurosporine (HY-15141)- and Doxorubicin (HY-15142)-evoked cell death on human neuroblastoma SH-SY5Y cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (225-250 g)[1]
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Dosage:10 mg/kg (Pharmacokinetic Analysis)
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Administration:Intraperitoneal injection
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Result:T1/2 (1.9 h).
Chemical Information
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No. CAS 1161205-04-4
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Appearance Solid
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Peso molecular 262.69
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Fòrmula C13H11ClN2O2
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Color White to off-white
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SMILES
ClC(C=C1)=C(OC)C=C1NC(C2=NC=CC=C2)=O
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Synonyms
ML-128
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 100 mg/mL (380.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 2 mg/mL (7.61 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Engers DW, et al. 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. [Content Brief]
[2]. Engers DW, et al. 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. [Content Brief]
[3]. Jantas D, et al. Neuroprotective effects of mGluR II and III activators against staurosporine- and doxorubicin-induced cellular injury in SH-SY5Y cells: New evidence for a mechanism involving inhibition of AIF translocation. Neurochem Int. 2015 Sep;88:124-37. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.8068 mL | 19.0338 mL | 38.0677 mL | 95.1692 mL |
| 5 mM | 0.7614 mL | 3.8068 mL | 7.6135 mL | 19.0338 mL | |
| 10 mM | 0.3807 mL | 1.9034 mL | 3.8068 mL | 9.5169 mL | |
| 15 mM | 0.2538 mL | 1.2689 mL | 2.5378 mL | 6.3446 mL | |
| 20 mM | 0.1903 mL | 0.9517 mL | 1.9034 mL | 4.7585 mL | |
| 25 mM | 0.1523 mL | 0.7614 mL | 1.5227 mL | 3.8068 mL | |
| 30 mM | 0.1269 mL | 0.6345 mL | 1.2689 mL | 3.1723 mL | |
| 40 mM | 0.0952 mL | 0.4758 mL | 0.9517 mL | 2.3792 mL | |
| 50 mM | 0.0761 mL | 0.3807 mL | 0.7614 mL | 1.9034 mL | |
| 60 mM | 0.0634 mL | 0.3172 mL | 0.6345 mL | 1.5862 mL | |
| 80 mM | 0.0476 mL | 0.2379 mL | 0.4758 mL | 1.1896 mL | |
| 100 mM | 0.0381 mL | 0.1903 mL | 0.3807 mL | 0.9517 mL |
VU0361737 Related Classifications
HY-14418 Related Classifications
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