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    Neuronal Signaling
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  3. ADX-47273

ADX-47273 

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

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

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
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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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Description

ADX-47273 is a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM). IC50 value: 170 nM(EC50) [1] [2] Target: positive allosteric modulator (PAM) of mGluR5 in vitro: ADX-47273 increased (9-fold) the response to threshold concentration of glutamate (50 nM) in fluorometric Ca(2+) assays (EC(50) = 170 nM) in human embryonic kidney 293 cells expressing rat mGlu5. ADX47273 dose-dependently shifted mGlu5 receptor glutamate response curve to the left (9-fold at 1 microM) and competed for binding of [(3)H]2-methyl-6-(phenylethynyl)pyridine (K(i) = 4.3 microM), but not [(3)H]quisqualate [2]. 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. In models sensitive to antipsychotic drug treatment, ADX47273 reduced rat-conditioned avoidance responding [minimal effective dose (MED) = 30 mg/kg i.p.] and decreased mouse apomorphine-induced climbing (MED = 100 mg/kg i.p.), with little effect on stereotypy or catalepsy [2]. ADX47273 had no effect on single-session and multi-session extinction, but administration of ADX47273 after a single retrieval trial enhanced subsequent fear extinction learning [3].

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.

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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

Purity: 99.34%

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ADX-47273
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