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ADX-47273

Catalog No. T2053 CAS 851881-60-2

Synonyms: BA 94673139

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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ADX-47273, CAS 851881-60-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 33.00
5 mg	In stock	$ 51.00
10 mg	In stock	$ 79.00
25 mg	In stock	$ 169.00
50 mg	In stock	$ 316.00
100 mg	In stock	$ 568.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 99.18%

Purity: 97%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	ADX-47273 (BA 94673139) is a positive and selective allosteric modulator for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM).
Targets&IC50	mGlu5:0.17 μM(EC50)
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.

Synonyms	BA 94673139
Molecular Weight	369.36
Formula	C20H17F2N3O2
CAS No.	851881-60-2

Storage

Powder: -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)

References and Literature

1. Liu F, et al. J Pharmacol Exp Ther, 2008, 327(3), 827-839. 2. Rosenbrock H, et al. Eur J Pharmacol, 2010, 639(1-3), 40-6. 3. Schlumberger C, et al. Pharmacol Biochem Behav, 2010, 95(1), 23-30.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Anti-Neurodegenerative Disease Compound Library Neurotransmitter Receptor Compound Library Target-Focused Phenotypic Screening Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Anti-Alzheimer's Disease Compound Library CNS-Penetrant Compound Library Fluorochemical Library Preclinical Compound Library

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L-AP4 LY382884 VU0650786 JNJ-46281222 CMPDA mGluR3 modulator-1 KM02894 LY2979165

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Keywords

ADX-47273 851881-60-2 Neuroscience GluR mGluR5 mGluR Inhibitor ADX 47273 glutamate BA94673139 antipsychotic inhibit procognitive ADX47273 BA 94673139 Metabotropic glutamate receptors BA-94673139 inhibitor

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