PCS1055

PCS1055 is a selective and competitive antagonist for muscarinic M4 receptor with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 is also an inhibitor for AChE with IC50 of 22 nM and 120 nM for electric eel and human AChE, respectively[1][2].

Product Specifications

CAS Number

[357173-55-8]

UNSPSC

12352005

Target

Cholinesterase (ChE) ; mAChR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/pcs1055.html

Purity

98.02

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

C12=NN=C(NCCC3CCN(CC4=CC=CC=C4)CC3)C=C1CCCC5=CC=CC=C52

Molecular Formula

C27H32N4

Molecular Weight

412.57

References & Citations

[1]Croy CH, et al. Characterization of PCS1055, a novel muscarinic M4 receptor antagonist. Eur J Pharmacol. 2016 Jul 5;782:70-6.|[2]Contreras JM, et al. Design, synthesis, and structure-activity relationships of a series of 3-[2- (1-benzylpiperidin-4-yl) ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors. J Med Chem. 2001 Aug 16;44 (17) :2707-18.