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Purity: ≥98%
ADX47273 (ADX-47273; BA-94673139; BA94673139) is a potent, selective and specific mGlu5 positive allosteric modulator(PAM) with important biological activity. It activates mGlu5 with an EC50 of 0.17 μM, and exhibits no activity against other mGlu subtypes. In vivo, ADX47273 increased extracellular signal-regulated kinase and cAMP-responsive element-binding protein phosphorylation in hippocampus and prefrontal cortex, both of which are critical for glutamate-mediated signal transduction mechanisms.
| ln Vitro |
In HEK 293 cells expressing rat mGlu5, ADX-47273 (0.1 nM-10 μM; 5 min) increases the response to 50 nM glutamate in a concentration-dependent manner without eliciting a response on its own[1]. With an EC50 of 0.23 μM, ADX-47273 (0.1 nM–10 μM; 5 min) increases the response to 300 nM glutamate in primary astrocyte cultures in a concentration-dependent manner[1]. With a Ki of 4.3 μM, ADX47273 (0.01-10 μM; 60 min) inhibits the binding of [3H]MPEP to the membranes of rat mGlu5 receptor-expressing HEK cells[1].
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| ln Vivo |
In rat hippocampal and prefrontal cortex, ADX47273 (1–10 mg/kg; single ip) increases phosphorylation of ERK and CREB in a dose-dependent manner[1]. Rats' conditioned avoidance response is reduced by ADX47273 (10-100 mg/kg; one ip) in a dose-dependent way[1]. In mice, apomorphine-induced climbing is inhibited by ADX47273 (10-300 mg/kg; ip)[1]. In rats, ADX47273 (0.1-50 mg/kg; ip) decreases impulsivity and improves recognition of novel objects in the five-choice serial reaction time test[1]. In mice using the Morris Water Maze (MWM), ADX47273 (15 mg/kg; ip) improves reversal learning[3].
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| Animal Protocol |
Animal/Disease Models: Male Long-Evans rats[1]
Doses: 1, 10 mg/kg Route of Administration: A single ip Experimental Results: Increased ERK and CREB phosphorylation in both the prefrontal cortex and hippocampus. |
| References |
[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
[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. [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. |
| Molecular Formula |
C20H17F2N3O2
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| Molecular Weight |
369.36
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| CAS # |
851881-60-2
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| Related CAS # |
(R)-ADX-47273;851881-59-9
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| SMILES |
FC1C([H])=C([H])C(=C([H])C=1[H])C(N1C([H])([H])C([H])([H])C([H])([H])[C@]([H])(C2=NC(C3C([H])=C([H])C(=C([H])C=3[H])F)=NO2)C1([H])[H])=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7074 mL | 13.5369 mL | 27.0739 mL | |
| 5 mM | 0.5415 mL | 2.7074 mL | 5.4148 mL | |
| 10 mM | 0.2707 mL | 1.3537 mL | 2.7074 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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