Free shipping on all orders over $ 500

ADX-47273

Cat. No. M3445
ADX-47273 Structure
Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 90  USD90 In stock
50mg USD 325  USD325 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

ADX-47273 is a novel, potent and selective metabotropic glutamate receptor 5 allosteric modulator with an EC50 of 170 nM in human embryonic kidney 293 cells expressing rat mGlu5. ADX-47273 shifted mGlu5 receptor glutamate response curve to the left (9-fold at 1 μM) and competed for binding of [3H]2-methyl-6- (phenylethynyl) pyridine with a Ki of 4.3 μM in a dose-dependent manner, but not [3H]quisqualate. In vivo, ADX-47273 elevated extracellular signal-regulated kinase and cAMP-responsive element-binding protein phosphorylation in hippocampus and prefrontal cortex. In models sensitive to antipsychotic compound treatment, ADX-47273 decreased rat-conditioned avoidance responding [minimal effective dose (MED) = 30 mg/kg i.p.] and reduced mouse apomorphine-induced climbing (MED = 100 mg/kg i.p.), with little effect on stereotypy or catalepsy. Furthermore, ADX-47273 inhibited phencyclidine, apomorphine, and amphetamine-induced locomotor activities in mice and reduced extracellular levels of dopamine in the nucleus accumbens, but not in the striatum, in rats. In cognition models, ADX-47273 improved novel object recognition (MED = 1 mg/kg i.p.) and decreased impulsivity in the five-choice serial reaction time test (MED = 10 mg/kg i.p.) in rats.

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models male Long-Evans rats
Formulation sterile 0.9% sodium chloride solution
Dosages 10 mg/kg
Administration Inject intraperitoneally at a single dose30 min before sacrifice
Chemical Information
Molecular Weight 369.36
Formula C20H17F2N3O2
CAS Number 851881-60-2
Solubility (25°C) DMSO 70 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Marta Marszalek-Grabska, et al. ADX-47273, a mGlu5 receptor positive allosteric modulator, attenuates deficits in cognitive flexibility induced by withdrawal from 'binge-like' ethanol exposure in rats

[2] Shaun R Stauffer. Progress toward positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5)

[3] Katja S Kroker, et al. Differential effect of the mGlu5 receptor positive allosteric modulator ADX-47273 on early and late hippocampal LTP

[4] Jeffrey P Lamb, et al. Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists

[5] Darren W Engers, et al. Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273

Related GluR Products
PDZ1 Domain inhibitor peptide

PDZ1 Domain inhibitor peptide, a cyclic peptide, incorporates a β-Ala lactam side chain linker and targets the PDZ1 domains of the postsynaptic density protein 95 (PSD-95).

CALP1

CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca2+-binding site.

NT 13

NT 13 (TPPT) is a tetrapeptide having the amino acid sequence L-threonyl-L-prolyl-L-prolyl-L-threonine amide.

Tat-NR2Baa

Tat-NR2BAA is the control peptide of Tat-NR2B9c, inactive.

VSGLNPSLWSIFGLQFILLWLVSGSRHYLW

VSGLNPSLWSIFGLQFILLWLVSGSRHYLW is a 30-amino-acid peptide mimicking the C-terminal domain of α2δ-1, termed as α2δ-1Tat peptide.

  Catalog
Abmole Inhibitor Catalog




Keywords: ADX-47273 supplier, GluR, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.