NAChR agonist 1

NAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR) . nAChR agonist 1 has the EC50 of 0.32 μM in a Ca2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease[1].

Product Specifications

CAS Number

[1394371-75-5]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

NAChR

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/nachr-agonist-1.html

Purity

98.35

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

NS(C1=CC=C(C2=C(C(CC)=O)SC(C3=CC=C(Cl)C=C3)=C2C)C=C1)(=O)=O

Molecular Formula

C20H18ClNO3S2

Molecular Weight

419.94

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[1]Sinha N, et al.Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptor [4- (5- (4-Chlorophenyl) -4-methyl-2-propionylthiophen-3-yl) benzenesulfonamide]: Structure-Activity Relationship and Preclinical Characterization. J Med Chem. 2020 Feb 13;63 (3) :944-960.