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PCS1055 dihydrochloride

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Catalog No. T16443Cas No. 361979-40-0

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

PCS1055 dihydrochloride

PCS1055 dihydrochloride

😃Good
Catalog No. T16443Cas No. 361979-40-0
PCS1055 dihydrochloride is an effective, selective, and competitive muscarinic M4 receptor antagonist (IC50: 18.1 nM and a Kd: 5.72 nM). PCS1055 dihydrochloride is also a potent AChE inhibitor (IC50 s: 22 nM and 120 nM for electric eel and human AChE, respectively). PCS1055 dihydrochloride inhibits radioligand [3H]-NMS binding to the M4 receptor (Ki: 6.5 nM). PCS1055 dihydrochloride shows >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor.
Pack SizePriceAvailabilityQuantity
25 mg$1,5206-8 weeks
50 mg$1,9806-8 weeks
100 mg$2,5006-8 weeks
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Product Introduction

Bioactivity
Description
PCS1055 dihydrochloride is an effective, selective, and competitive muscarinic M4 receptor antagonist (IC50: 18.1 nM and a Kd: 5.72 nM). PCS1055 dihydrochloride is also a potent AChE inhibitor (IC50 s: 22 nM and 120 nM for electric eel and human AChE, res
Targets&IC50
M4 mAChR:(kd)5.72 nM, M4 mAChR:18.1 nM
In vitro
PCS1055 effectively inhibits G protein activation in a concentration-dependent manner, demonstrating its highest potency at M4 receptors. Research indicates that PCS1055 shows a pronounced binding and functional preference for the M4 receptor subtype, surpassing its affinity and effectiveness for M1-, M2-, M3-, and M5 receptors by 130-, 31.2-, 426-, and >1000-fold, and 255-, 69.1-, 342-, and >1000-fold, respectively. Furthermore, PCS1055 counteracts functional signal transduction, evidenced by its ability to inhibit agonist-stimulated GTP-γ-[35S] binding, showcasing its antagonistic properties.
In vivo
PCS1055 (30 mg/kg; intraperitoneal injection; male mice) treatment achieves peak plasma levels at 30 minutes, with total and unbound plasma concentrations of 45100 nM and 631 nM, respectively. At 1 hour, maximal brain exposure of the compound is observed at 11.8 nM [1].
Chemical Properties
Molecular Weight485.49
FormulaC27H34Cl2N4
Cas No.361979-40-0
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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