This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
PCS1055 dihydrochloride
Catalog No. T16443 CAS
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.
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage
& Solubility Information
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, 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.
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 displays the maximal plasma levels at the 30 min time-point with 45100 nM total and 631nM unbound plasma concentrations. At 1 h, the maximal compound exposure observed in the brain is 11.8 nM [1].
Molecular Weight
485.49
Formula
C27H34Cl2N4
CAS No.
361979-40-0
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL Corn oil,mix and clarify.
Note:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.