Foliglurax
Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 79 nM. Antiparkinsonian effect.
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- CAS No.: 1883329-51-8
- Formule: C23H23N3O3S
- Masse moléculaire:421.51
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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mGlu4 79 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
>15 μM
Compound: 60; PXT002331
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Positive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing chimeric G protein assessed as increase in glutamate-induced calcium flux after 10 mins by Fluo4-AM dye based fluorescence assay
Positive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing chimeric G protein assessed as increase in glutamate-induced calcium flux after 10 mins by Fluo4-AM dye based fluorescence assay
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[PMID: 28902994] |
| HEK293 | EC50 |
79 nM
Compound: 60; PXT002331
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Positive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing Gi/Gq assessed as increase in glutamate-induced calcium flux preincubated for 10 mins followed by glutamate addition measured for 3 mins by Fluo4-AM
Positive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing Gi/Gq assessed as increase in glutamate-induced calcium flux preincubated for 10 mins followed by glutamate addition measured for 3 mins by Fluo4-AM
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[PMID: 28902994] |
Foliglurax, a highly selective and potent mGlu4 receptor PAM with a marked brain-penetrance feature, might revolutionize the field of mGlu4 receptor drug targeting in CNS disorders[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1883329-51-8
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Masse moléculaire 421.51
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Formule C23H23N3O3S
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SMILES
O/N=C1C=C(C2=CC3=C(C=CS3)C=N2)OC4=CC=C(CCCN5CCOCC5)C=C\14
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Synonyms
PXT002331
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvant et solubilité
DMSO : 5.2 mg/mL (12.34 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.52 mg/mL (1.23 mM); Clear solution
This protocol yields a clear solution of ≥ 0.52 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.52 mg/mL (1.23 mM); Clear solution
This protocol yields a clear solution of ≥ 0.52 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureté et documentation
Références
[1]. Charvin D, et al. Discovery, Structure-Activity Relationship, and Antiparkinsonian Effect of a Potent and Brain-Penetrant Chemical Series of Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4. J Med Chem. 2017 Oct 26;60(20):8515-8537. [Content Brief]
[2]. Volpi C, et al. Opportunities and challenges in drug discovery targeting metabotropic glutamate receptor 4. Expert Opin Drug Discov. 2018 May;13(5):411-423. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3724 mL | 11.8621 mL | 23.7242 mL | 59.3106 mL |
| 5 mM | 0.4745 mL | 2.3724 mL | 4.7448 mL | 11.8621 mL | |
| 10 mM | 0.2372 mL | 1.1862 mL | 2.3724 mL | 5.9311 mL |
Foliglurax Related Classifications
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