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PZ0135 Sigma-Aldrich

PHA-543613

≥98% (HPLC)

Synonym: N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide

  • CAS Number 478149-53-0

  • Empirical Formula (Hill Notation) C15H17N3O2

  • Molecular Weight 271.31

  •  PubChem Substance ID 329823720

  •  NACRES NA.77

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Properties

Related Categories Agonists, Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology,
Quality Level   100
assay   ≥98% (HPLC)
form   powder
mfr. no.   Pfizer®
color   white to off-white
solubility   DMSO: ≥20 mg/mL
originator   Pfizer
storage temp.   room temp
SMILES string   O=C(N[C@H]1CN2CC[C@H]1CC2)c3cc4ccoc4cn3
InChI   1S/C15H17N3O2/c19-15(12-7-11-3-6-20-14(11)8-16-12)17-13-9-18-4-1-10(13)2-5-18/h3,6-8,10,13H,1-2,4-5,9H2,(H,17,19)/t13-/m0/s1
InChI key   IPKZCLGGYKRDES-ZDUSSCGKSA-N
Gene Information   human ... CHRNA7(1139)

Description

Application

PHA-543613 has been used to study its effect on recognition memory and neurovascular coupling (NVC) response in β-amyloid (Aβ) 25-35-treated mice. It has also been used to study its effect on Aβ25-35-induced receptor alteration and cognitive impairment in mice.

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

PHA-543613 exhibits rapid brain penetration property.

PHA-543613 is a potent selective α7 nAChR agonist. Nicotinic acetylcholine receptors are ligand-gated ion channels activated by nicotine, expressed in multiple tissues, with high functional expression in brain. The homomeric subtype α7 is a potential therapeutic target for cognitive deficits in schizophrenia and Alzheimer′s disease. PHA-543613 is active in both in vitro (binding, calcium flux, patch-clamp) and in vivo (auditory gating, novel object recognition) assays.

Features and Benefits

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®Pfizer), a collection of 90 Pfizer-developed drugs and research tools. Click here to learn more.

This compound is featured on the Acetylcholine Receptors (Nicotinic) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Other Notes

This compound was developed by Pfizer for Neuroscience research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.

To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

LOPAC is a registered trademark of Sigma-Aldrich Co. LLC

Pfizer is a registered trademark of Pfizer, Inc.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
WGK 1
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles

Articles

Acetylcholine Receptors (Nicotinic)

Nicotinic acetylcholine receptors (nAChRs) constitute a family of ligand-gated channels, originally classified on the basis of their activation by the alkaloid nicotine, with acetylcholine (ACh) bein...
Keywords: Analgesics, Diseases, Dopamine agents, Gene expression, Genetic, Inflammation, Ligands, Microscopy, Neurotransmission, Neurotransmitters, Scanning electron microscopy, Schizophrenia, Tissue microarrays, Transduction

Pfizer Compounds for Neuroscience

From our library of Articles, Sigma-Aldrich presents Pfizer Compounds for Neuroscience

Peer-Reviewed Papers
15

References

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