1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. ADX-47273

ADX-47273 

Cat. No.: HY-13058 Purity: 99.34%
Handling Instructions

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.

For research use only. We do not sell to patients.

ADX-47273 Chemical Structure

ADX-47273 Chemical Structure

CAS No. : 851881-60-2

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
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50 mg USD 348 In-stock
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100 mg USD 624 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1][2].

IC50 & Target[1]

mGluR5

0.17 μM (EC50)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

ADX47273 (1-10 mg/kg; a single i.p.) dose-dependently increases ERK and CREB phosphorylation in rat hippocampus and prefrontal cortex[1].
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Long-Evans rats[1]
Dosage: 1, 10 mg/kg
Administration: A single i.p.
Result: Increased ERK and CREB phosphorylation in both the prefrontal cortex and hippocampus.
Molecular Weight

369.36

Formula

C₂₀H₁₇F₂N₃O₂

CAS No.

851881-60-2

SMILES

O=C(C1=CC=C(F)C=C1)N2C[[email protected]@H](C3=NC(C4=CC=C(F)C=C4)=NO3)CCC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (83.93 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

ADX-47273ADX47273ADX 47273mGluRMetabotropic glutamate receptorsmGluR5glutamateantipsychoticprocognitiveInhibitorinhibitorinhibit

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ADX-47273
Cat. No.:
HY-13058
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