ADX 47273

SKU: orb1223854

Description

ADX-47273 is a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM).

Research Area

Metabolism Research

Key Properties

• CAS Number: 851881-60-2
• MW: 369.36
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₇F₂N₃O₂
• SMILES: O=C(C1=CC=C(F)C=C1)N2C[C@@H](C3=NC(C4=CC=C(F)C=C4)=NO3)CCC2
• Target: GluR
• Solubility: Ethanol: 30 mg/mL (81.22 mM); DMSO: 74 mg/mL (200.34 mM)

Bioactivity

• In Vivo:
  ADX47273 (1-10 mg/kg; a single i.p.) dose-dependently increases ERK and CREB phosphorylation in rat hippocampus and prefrontal cortex. ADX47273 (10-100 mg/kg; a single i.p.) decreases conditioned avoidance responding in a dose-dependent manner in rats. ADX47273 (10-300 mg/kg; i.p.) blocks apomorphine-induced climbing in mice. 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. ADX47273 (15 mg/kg; i.p.) enhances reversal learning in the Morris Water Maze (MWM) in mice. Animal model: Male Long-Evans rats. Dosage: 1, 10 mg/kg. Administration: A single i.p. Result: Increased ERK and CREB phosphorylation in both the prefrontal cortex and hippocampus.
• 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. 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ADX-47273 | ADX 47273 | ADX47273

Quick Database Links

Gene Symbol

GluR