PHA 568487 CAS: 527680-56-4
MF: C16H20N2O3•C4H4O4
MW: 404.41
An agonist of AChR α7.

PHA 568487 (CAS 527680-56-4)

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Alternate Names: N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl- 2,3-dihydro-1,4-benzodioxin-6-carboxamide fumarate
Application: PHA 568487 is an agonist of AChR α7
CAS Number: 527680-56-4
Molecular Weight: 404.41
Molecular Formula: C16H20N2O3•C4H4O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

PHA 568487 is an agonist of AChR α7 (Ki values are 44 and 2800 for α7 and 5-HT3, respectively, IC50 values are > 100 µM for α3β4 and α1β1δγ, respectively, and % inhibition is < 1 and 5 % for α4β2 and hERG, respectively). It is orally active and a brain penetrant.


References

Walker et al (2006) Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as a7 nicotinic acetylcholine receptor agonists. Bioorg.Med.Chem. 14 8219.

Physical State :
Solid
Solubility :
Soluble in water (100 mM), and DMSO (100 mM).
Storage :
Desiccate at room temperature
Refractive Index :
n20D ~1.62 (Predicted)
Optical Activity :
α20/D +4.2°, c = 0.9 in methanol
IC50 :
Neuronal acetylcholine receptor protein α-7 subunit: EC5050 = 36.2 nM (rat); α3β4: IC50 > 100 µM; α1β1δγ: IC50 > 100 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
57350525
MDL Number :
MFCD11519961
SMILES :
C1CN2CCC1[[email protected]](C2)NC(=O)C3=CC4=C(C=C3)OCCO4.C(=CC(=O)O)C(=O)O

Download SDS (MSDS)

Certificate of Analysis

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