RO0711401
Based on 2 publication(s) in Google Scholar
RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.35%
- No. CAS: 714971-87-6
- Fòrmula: C18H11F3N2O3
- Peso molecular:360.29
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Publications Citing Use of MedChemExpress (MCE) RO0711401
More
Actividad biológica
Descripciòn
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mGluR1 56 nM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
202 nM
Compound: 14a
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Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
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[PMID: 19233648] |
| HEK293 | EC50 |
56 nM
Compound: 14a
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Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
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[PMID: 19233648] |
In Vivo
Systemic injection of RO0711401 is shown to reduce the frequency of spike-and-wave discharges in a rat model of absence epilepsy, and to improve motor signs in autoimmune encephalomyelitis (EAE) mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Spinocerebellar ataxia type 1 (SCA1) mice (30-week old)[1]
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Dosage:10 mg/kg
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Administration:Subcutaneous injection; once
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Result:Caused a prolonged improvement of motor performance on the rotarod and the paw-print tests.
Chemical Information
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No. CAS 714971-87-6
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Appearance Solid
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Peso molecular 360.29
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Fòrmula C18H11F3N2O3
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Color White to off-white
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SMILES
O=C(NC1=NC(C(F)(F)F)=CO1)C2C3=C(C=CC=C3)OC4=C2C=CC=C4
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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 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Death Discov
Preso enhances mGluR1-mediated excitotoxicity by modulating the phosphorylation of mGluR1-Homer1 complex and facilitating an ER stress after traumatic brain injury. [Abstract]2024 Mar 26;10(1):153. PMID: 38531909 -
Neurobiol Dis
Impedance-based phenotypic profiling of metabotropic glutamate receptor ligand responses in SCA1 human iPSC-derived neuronal cultures. [Abstract]2026 Mar:220:107296. PMID: 41620186
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (277.55 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
In Vivo Dissolution Calculator
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 (277 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]. Serena Notartomaso, et al. Pharmacological enhancement of mGlu1 metabotropic glutamate receptors causes a prolonged symptomatic benefit in a mouse model of spinocerebellar ataxia type 1. Mol Brain. 2013 Nov 19;6:48. [Content Brief]
[2]. Eric Vieira, et al. Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1666-9. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7755 mL | 13.8777 mL | 27.7554 mL | 69.3885 mL |
| 5 mM | 0.5551 mL | 2.7755 mL | 5.5511 mL | 13.8777 mL | |
| 10 mM | 0.2776 mL | 1.3878 mL | 2.7755 mL | 6.9389 mL | |
| 15 mM | 0.1850 mL | 0.9252 mL | 1.8504 mL | 4.6259 mL | |
| 20 mM | 0.1388 mL | 0.6939 mL | 1.3878 mL | 3.4694 mL | |
| 25 mM | 0.1110 mL | 0.5551 mL | 1.1102 mL | 2.7755 mL | |
| 30 mM | 0.0925 mL | 0.4626 mL | 0.9252 mL | 2.3130 mL | |
| 40 mM | 0.0694 mL | 0.3469 mL | 0.6939 mL | 1.7347 mL | |
| 50 mM | 0.0555 mL | 0.2776 mL | 0.5551 mL | 1.3878 mL | |
| 60 mM | 0.0463 mL | 0.2313 mL | 0.4626 mL | 1.1565 mL | |
| 80 mM | 0.0347 mL | 0.1735 mL | 0.3469 mL | 0.8674 mL | |
| 100 mM | 0.0278 mL | 0.1388 mL | 0.2776 mL | 0.6939 mL |
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