1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
    AChE
  3. PCS1055 dihydrochloride

PCS1055 dihydrochloride 

Cat. No.: HY-122203
Handling Instructions

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.

For research use only. We do not sell to patients.

PCS1055 dihydrochloride Chemical Structure

PCS1055 dihydrochloride Chemical Structure

CAS No. : 361979-40-0

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Description

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].

IC50 & Target

IC50: 18.1 nM (Muscarinic M4 receptor); Kd: 5.72 nM (Muscarinic M4 receptor)[1];
IC50: 22 nM (Electric eel AChE) and 120 nM (Human AChE)[2]

In Vitro

PCS1055 also antagonized functional signal transduction as demonstrates by the inhibition of agonist-stimulated GTP-γ-[35S] binding. PCS1055 inhibits G protein activation in a concentration dependent manner, with the highest potency at the M4 receptors. Both studies shows that PCS1055 is most potent at the M4 receptor subtype with a binding preference of 130-, 31.2-, 426- and >1000-fold, and functional preference of 255-, 69.1-, 342- and >1000-fold over the M1-, M2-, M3- and M5 receptors, respectively[1].

In Vivo

PCS1055 (30 mg/kg; intraperitoneal injection; male mice) treatment shows the maximal plasma levels at the 30 min time-point with 45100 nM total and 631nM unbound plasma concentrations. The maximal compound exposure observed in the brain is 11.8 nM at 1 h[1].

Animal Model: Male mice[1]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection (Pharmacokinetic Analysis)
Result: The maximal plasma levels were observed at the 30 min time-point with 45100 nM total and 631nM unbound plasma concentrations. The maximal compound exposure observed in the brain was 11.8 nM at 1 h.
Molecular Weight

485.49

Formula

C₂₇H₃₄Cl₂N₄

CAS No.

361979-40-0

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PCS1055PCS 1055PCS-1055mAChRAChEMuscarinic acetylcholine receptorAcetylcholinesteraseFunctionalG-proteinactivationmuscarinicM4receptorelectriceelInhibitorinhibitorinhibit

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PCS1055 dihydrochloride
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