For research use only. Not for therapeutic Use.
PCS1055 dihydrochloride(CAT: I011979) is a potent, selective, and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. It inhibits [³H]-NMS binding with a Ki of 6.5 nM and demonstrates exceptional selectivity (>100-fold over M1, M3, M5; 30-fold over M2). PCS1055 also acts as a dual acetylcholinesterase (AChE) inhibitor, with IC50 values of 22 nM (eel AChE) and 120 nM (human AChE). Functionally, it antagonizes agonist-stimulated GTP-γ-[³⁵S] binding, showing the highest potency at M4. In vivo, intraperitoneal dosing (30 mg/kg) yields significant plasma and brain exposure, supporting its use in neurological disease research.
CAS Number | 361979-40-0 |
Synonyms | N-[2-(1-benzylpiperidin-4-yl)ethyl]-3,4-diazatricyclo[9.4.0.02,7]pentadeca-1(15),2,4,6,11,13-hexaen-5-amine;dihydrochloride |
Molecular Formula | C27H34Cl2N4 |
Purity | ≥95% |
IUPAC Name | N-[2-(1-benzylpiperidin-4-yl)ethyl]-3,4-diazatricyclo[9.4.0.02,7]pentadeca-1(15),2,4,6,11,13-hexaen-5-amine;dihydrochloride |
InChI | InChI=1S/C27H32N4.2ClH/c1-2-7-22(8-3-1)20-31-17-14-21(15-18-31)13-16-28-26-19-24-11-6-10-23-9-4-5-12-25(23)27(24)30-29-26;;/h1-5,7-9,12,19,21H,6,10-11,13-18,20H2,(H,28,29);2*1H |
InChIKey | VSCSFYDNGYAWKG-UHFFFAOYSA-N |
SMILES | C1CC2=CC=CC=C2C3=NN=C(C=C3C1)NCCC4CCN(CC4)CC5=CC=CC=C5.Cl.Cl |
Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |