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PCS1055 (dihydrochloride)

PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively[1][2].

Product Specifications

CAS Number

[361979-40-0]

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-dihydrochloride.html

Purity

98.88

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

[H]Cl.[H]Cl.C12=NN=C(NCCC3CCN(CC4=CC=CC=C4)CC3)C=C1CCCC5=CC=CC=C52

Molecular Formula

C27H34Cl2N4

Molecular Weight

485.49

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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

AChE; mAChR4

Citation 01

Neuron. 2025 Mar 5;113 (5) :670-683.e7.|Mol Cell Endocrinol. 2025 Jan 21:599:112464.

Available Sizes

Curated Selection

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