Free shipping on all orders over $ 500

ADX-47273

Cat. No. M3445
ADX-47273 Structure
Size Price Availability Quantity
5mg USD 180 In stock
10mg USD 300 In stock
50mg USD 900 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 369.36
Formula C20H17F2N3O2
CAS Number 851881-60-2
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
Related GluR Products
Lu AF21934

Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4.

Beclometasone dipropionate

Beclomethasone dipropionate is a potent glucocorticoid steroid used for the treatment of rhinitis and sinusitis.

(-)-Huperzine A

(-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4.

TCN-201

TCN 201 is a NMDA receptor antagonist for NR1/NR2A and NR1/NR2B with pIC50 of 6.8 and 4.3, respectively.

VU 0357121

VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ADX-47273 supplier, GluR, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.