TargetMol

PCS1055 dihydrochloride

Product Code:
 
TAR-T16443
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T16443-5mg5mg£850.00
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TAR-T16443-50mg50mg£1,661.00
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TAR-T16443-100mg100mg£2,079.00
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Further Information

Bioactivity:
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.
CAS:
361979-40-0
Formula:
C27H34Cl2N4
Molecular Weight:
485.5
Purity:
0.98
SMILES:
Cl.Cl.C(CC1CCN(Cc2ccccc2)CC1)Nc1cc2CCCc3ccccc3-c2nn1

References

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.