ADX88178
Based on 1 publication(s) in Google Scholar
ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
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- Pureté: 99.50%
- CAS No.: 1235318-89-4
- Formule: C12H12N6S
- Masse moléculaire:272.33
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) ADX88178
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Activité biologique
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mGluR4 4 nM (EC50) |
ADX88178 is developed as a potent and selective mGluR4 positive allosteric modulator. ADX88178 is used as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4). ADX88178 potentiates glutamate-mediated activation of human mGluR4 with EC50 values of 4 nM without significant effects on other mGluRs (EC50 > 30 μM)[1]. ADX88178 is novel potent, selective, and brain-penetrant positive allosteric modulator of the mGlu4. Microglia are pretreated with 1, 10 or 100 nM ADX88178 or 100 nM LAP4 for 30 min followed by LPS treatment for 24 h prior to collecting culture supernatant for ELISA measurement of TNFα levels. The pre-treatment with ADX88178 and LAP4 both significantly attenuate LPS-induced TNFα levels. As little as 1 nM of ADX88178 is sufficient to inhibit TNFα, and is as effective at concentrations of 10 and 100 nM[2].
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.
Chemical Information
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CAS No. 1235318-89-4
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Appearance Solid
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Masse moléculaire 272.33
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Formule C12H12N6S
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Color Light yellow to yellow
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SMILES
CC1=C(C2=CNN=C2)N=C(NC3=NC=CC(C)=N3)S1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Res
Structural insights into dimerization and activation of the mGlu2-mGlu3 and mGlu2-mGlu4 heterodimers. [Abstract]2023 Oct;33(10):762-774. PMID: 37286794
Solvant et solubilité
DMSO : 16.67 mg/mL (61.21 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (6.13 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
Protocole
After adhesion to the chamber slides, microglia from WT and mGlu4 KO microglia pre-treated with 1 nM, 10 nM, 100 nM ADX88178, or 100 nM L-AP4. Each treatment is performed in quadruplicate. Thirty minutes after treatment with ADX88178 or L-AP4, 100 ng/mL LPS is added to the cultures and the cells are incubated at 37 °C for an additional 24 h. At the end of the 24 h treatment period, media is collected and analyzed for TNFα, and the cells are for iNOS and MHC II expression by immunocytochemistry[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice and Rats[3] Male mice (n=8-10/group) are treated orally (p.o.) via gavage with vehicle [1% carboxymethyl cellulose (CMC)], ADX88178 (1, 3, 10 and 30 mg/kg) or Diazepam (1.5 mg/kg). Male rats (n=10/group) are treated p.o. with vehicle (1% CMC), ADX88178 (10, 30, and 100 mg/kg), or Diazepam (3 mg/kg). After 60 minutes, animals are individually placed in the center of the maze (facing one of the closed arms) and left to explore for 5 minutes. A terminal blood sample is collected from all ADX88178-treated animals at the end of the experiment, and plasma is analyzed for the pharmacokinetic studies. The number of open-arm and closed-arm entries, as well as the time (seconds) spent in the open arms of the maze, is analyzed by one-way analysis of variance followed by Dunnett’s test.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (279 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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Instruction de manipulation (2659 KB)
Références
[1]. Fujinaga M, et al. Radiosynthesis and evaluation of 5-methyl-N-(4-[(11)C]methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine ([(11)C]ADX88178) as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4). Bioorg Med Chem L [Content Brief]
[2]. Ponnazhagan R, et al. The Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator ADX88178 Inhibits Inflammatory Responses in Primary Microglia. J Neuroimmune Pharmacol. 2016 Jun;11(2):231-7. [Content Brief]
[3]. Kalinichev M, et al. Characterization of the novel positive allosteric modulator of the metabotropic glutamate receptor 4 ADX88178 in rodent models of neuropsychiatric disorders. J Pharmacol Exp Ther. 2014 Sep;350(3):495-505. [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 | 3.6720 mL | 18.3601 mL | 36.7202 mL | 91.8004 mL |
| 5 mM | 0.7344 mL | 3.6720 mL | 7.3440 mL | 18.3601 mL | |
| 10 mM | 0.3672 mL | 1.8360 mL | 3.6720 mL | 9.1800 mL | |
| 15 mM | 0.2448 mL | 1.2240 mL | 2.4480 mL | 6.1200 mL | |
| 20 mM | 0.1836 mL | 0.9180 mL | 1.8360 mL | 4.5900 mL | |
| 25 mM | 0.1469 mL | 0.7344 mL | 1.4688 mL | 3.6720 mL | |
| 30 mM | 0.1224 mL | 0.6120 mL | 1.2240 mL | 3.0600 mL | |
| 40 mM | 0.0918 mL | 0.4590 mL | 0.9180 mL | 2.2950 mL | |
| 50 mM | 0.0734 mL | 0.3672 mL | 0.7344 mL | 1.8360 mL | |
| 60 mM | 0.0612 mL | 0.3060 mL | 0.6120 mL | 1.5300 mL |
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