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ADX-47273

ADX-47273
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Purity:99.18%
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ADX-47273

Catalog No. T2053Cas No. 851881-60-2
ADX-47273 (BA 94673139) is a positive and selective allosteric modulator for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM).
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Pack SizePriceAvailabilityQuantity
2 mg$33In Stock
5 mg$51In Stock
10 mg$79In Stock
25 mg$169In Stock
50 mg$316In Stock
100 mg$568In Stock
1 mL x 10 mM (in DMSO)$54In Stock
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Product Introduction

Bioactivity
Description
ADX-47273 (BA 94673139) is a positive and selective allosteric modulator for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM).
In vitro
Intraperitoneal administration of ADX47273 at a dosage of 10 mg/kg was found to increase the levels of ERK and CREB phosphorylation in the prefrontal cortex and hippocampus of Long-Evans rats. This effect was consistently observed with the same dosage. Moreover, intraperitoneal injections of ADX47273 at 100 mg/kg significantly reduced the conditioned avoidance response in Sprague-Dawley rats at both 30 and 90 minutes after administration. At a higher dosage of 175 mg/kg, ADX47273 was able to decrease dopamine levels in the nucleus accumbens of Sprague-Dawley rats.
In vivo
In HEK293 cells expressing rat mGlu5, ADX47273 at concentrations of 0.1 or 1 μM reduced the EC50 of glutamate by fourfold and ninefold, respectively. At a concentration of 0.3 μM, ADX-47273 induced NMDA receptor-dependent long-term potentiation in rat hippocampal slices, an effect that could be blocked by the specific mGlu5 receptor antagonist MPEP at 10 μM. In primary cultures of astrocytes, ADX47273 at concentrations of 1 or 3 μM reduced the EC50 of glutamate by four- and ninefold, respectively. ADX47273 elicited a concentration-dependent increase in the response to 50 nM glutamate in HEK293 cells expressing rat mGlu5, with the maximum enhancement approximately ninefold and an EC50 of 0.17±0.03 μM. ADX47273 inhibited the binding of [3H]MPEP to the cell membranes from HEK293 cells expressing the mGlu5 receptor, with a Ki of 4.3 ± 0.5 μM.
AliasBA 94673139
Chemical Properties
Molecular Weight369.36
FormulaC20H17F2N3O2
Cas No.851881-60-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
Ethanol: 28 mg/mL (75.8 mM)
DMSO: 69 mg/mL (186.8 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM2.7074 mL13.5369 mL27.0739 mL135.3693 mL
5 mM0.5415 mL2.7074 mL5.4148 mL27.0739 mL
10 mM0.2707 mL1.3537 mL2.7074 mL13.5369 mL
20 mM0.1354 mL0.6768 mL1.3537 mL6.7685 mL
50 mM0.0541 mL0.2707 mL0.5415 mL2.7074 mL
DMSO
1mg5mg10mg50mg
100 mM0.0271 mL0.1354 mL0.2707 mL1.3537 mL

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