ADX-47273
Based on 1 publication(s) in Google Scholar
ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC50 of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities.
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- Pureza: 98.77%
- No. CAS: 851881-60-2
- Fòrmula: C20H17F2N3O2
- Peso molecular:369.36
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) ADX-47273
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Actividad biológica
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mGluR5 0.17 μM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCCLM3 | IC50 |
66.4 μM
Compound: ADX-47273
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Antiproliferative activity against human HCCLM3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human HCCLM3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 38905539] |
| HEK293 | EC50 |
157 nM
Compound: 7, ADX-47273
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Positive allosteric modulation of human mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay
Positive allosteric modulation of human mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay
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[PMID: 24050755] |
| HEK293 | EC50 |
199 nM
Compound: 2, ADX47273
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Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay
Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay
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[PMID: 23947773] |
| HEK293 | EC50 |
55 nM
Compound: 7, ADX-47273
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Positive allosteric modulation of rat mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay
Positive allosteric modulation of rat mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay
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[PMID: 24050755] |
ADX-47273 (0.1 nM-10 μM; 5 min) causes a concentration-dependent increase in the response to 50 nM glutamate in HEK 293 cells expressing rat mGlu5 without eliciting a response by itself[1].
ADX-47273 (0.1 nM-10 μM; 5 min) causes a concentration-dependent increase in the response to 300 nM glutamate in primary astrocyte cultures, with an EC50 of 0.23 μM[1].
ADX47273 (0.01-10 μM; 60 min) inhibits [3H]MPEP binding to rat mGlu5 receptor HEK cell membranes, with a Ki of 4.3 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ADX47273 (10-100 mg/kg; a single i.p.) decreases conditioned avoidance responding in a dose-dependent manner in rats[1].
ADX47273 (10-300 mg/kg; i.p.) blocks apomorphine-induced climbing in mice[1].
ADX47273 (0.1-50 mg/kg; i.p.) increases novel object recognition and reduces impulsivity in the five-choice serial reaction time test in rats[1].
ADX47273 (15 mg/kg; i.p.) enhances reversal learning in the Morris Water Maze (MWM) in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Long-Evans rats[1]
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Dosage:1, 10 mg/kg
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Administration:A single i.p.
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Result:Increased ERK and CREB phosphorylation in both the prefrontal cortex and hippocampus.
Chemical Information
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No. CAS 851881-60-2
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Appearance Solid
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Peso molecular 369.36
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Fòrmula C20H17F2N3O2
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Color White to off-white
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SMILES
O=C(C1=CC=C(F)C=C1)N2C[C@@H](C3=NC(C4=CC=C(F)C=C4)=NO3)CCC2
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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
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
Methanol : 105.5 mg/mL (285.63 mM; Need ultrasonic and warming)
DMSO : ≥ 31 mg/mL (83.93 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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 (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Liu F, et al. ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and procognitive activities. J Pharmacol Exp Ther. 2008 Dec;327(3):827-39. [Content Brief]
[2]. Schlumberger C, et, al. Effects of a positive allosteric modulator of mGluR5 ADX47273 on conditioned avoidance response and PCP-induced hyperlocomotion in the rat as models for schizophrenia. Pharmacol Biochem Behav. 2010 Mar;95(1):23-30. [Content Brief]
[3]. Xu J, et al. Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning. Learn Mem. 2013 Jul 18;20(8):438-45. [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 / Methanol | 1 mM | 2.7074 mL | 13.5369 mL | 27.0739 mL | 67.6846 mL |
| 5 mM | 0.5415 mL | 2.7074 mL | 5.4148 mL | 13.5369 mL | |
| 10 mM | 0.2707 mL | 1.3537 mL | 2.7074 mL | 6.7685 mL | |
| 15 mM | 0.1805 mL | 0.9025 mL | 1.8049 mL | 4.5123 mL | |
| 20 mM | 0.1354 mL | 0.6768 mL | 1.3537 mL | 3.3842 mL | |
| 25 mM | 0.1083 mL | 0.5415 mL | 1.0830 mL | 2.7074 mL | |
| 30 mM | 0.0902 mL | 0.4512 mL | 0.9025 mL | 2.2562 mL | |
| 40 mM | 0.0677 mL | 0.3384 mL | 0.6768 mL | 1.6921 mL | |
| 50 mM | 0.0541 mL | 0.2707 mL | 0.5415 mL | 1.3537 mL | |
| 60 mM | 0.0451 mL | 0.2256 mL | 0.4512 mL | 1.1281 mL | |
| 80 mM | 0.0338 mL | 0.1692 mL | 0.3384 mL | 0.8461 mL | |
| Methanol | 100 mM | 0.0271 mL | 0.1354 mL | 0.2707 mL | 0.6768 mL |
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