Product Name :
PCS1055 dihydrochloride
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.
CAS:
361979-40-0
Molecular Weight:
485.49
Formula:
C27H34Cl2N4
Chemical Name:
N-[2-(1-benzylpiperidin-4-yl)ethyl]-3,4-diazatricyclo[9.4.0.0²,⁷]pentadeca-1(15),2(7),3,5,11,13-hexaen-5-amine dihydrochloride
Smiles :
Cl.Cl.C(C1C=CC=CC=1)N1CCC(CCNC2=CC3CCCC4=CC=CC=C4C=3N=N2)CC1
InChiKey:
VSCSFYDNGYAWKG-UHFFFAOYSA-N
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
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.{{Chenodeoxycholic Acid} medchemexpress|{Chenodeoxycholic Acid} Autophagy|{Chenodeoxycholic Acid} Biological Activity|{Chenodeoxycholic Acid} In Vivo|{Chenodeoxycholic Acid} manufacturer|{Chenodeoxycholic Acid} Cancer} 1 nM and a Kd of 5.{{Milvexian} medchemexpress|{Milvexian} Metabolic Enzyme/Protease|{Milvexian} Purity & Documentation|{Milvexian} In stock|{Milvexian} supplier|{Milvexian} Autophagy} 72 nM.PMID:23329319 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.|Product information|CAS Number: 361979-40-0|Molecular Weight: 485.49|Formula: C27H34Cl2N4|Chemical Name: N-[2-(1-benzylpiperidin-4-yl)ethyl]-3,4-diazatricyclo[9.4.0.0²,⁷]pentadeca-1(15),2(7),3,5,11,13-hexaen-5-amine dihydrochloride|Smiles: Cl.Cl.C(C1C=CC=CC=1)N1CCC(CCNC2=CC3CCCC4=CC=CC=C4C=3N=N2)CC1|InChiKey: VSCSFYDNGYAWKG-UHFFFAOYSA-N|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|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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.|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.|Products are for research use only. Not for human use.|