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MedKoo Cat#: 561488 | Name: PCS1055
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PCS1055 is a muscarinic M4 receptor antagonist. PCS1055 represents a new M4-preferring antagonist that may be useful in elucidating the roles of M4 receptor signaling.

Chemical Structure

PCS1055
PCS1055
CAS#361979-40-0

Theoretical Analysis

MedKoo Cat#: 561488

Name: PCS1055

CAS#: 361979-40-0

Chemical Formula: C27H34Cl2N4

Exact Mass: 0.0000

Molecular Weight: 485.50

Elemental Analysis: C, 66.80; H, 7.06; Cl, 14.60; N, 11.54

Price and Availability

Size Price Availability Quantity
5mg USD 425.00
25mg USD 850.00
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Related CAS #
No Data
Synonym
PCS1055; PCS-1055; PCS 1055;
IUPAC/Chemical Name
[2-(1-Benzyl-piperidin-4-yl)-ethyl]-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-amine Dihydrochloride
InChi Key
VSCSFYDNGYAWKG-UHFFFAOYSA-N
InChi Code
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
SMILES Code
[H]Cl.[H]Cl.C12=NN=C(NCCC3CCN(CC4=CC=CC=C4)CC3)C=C1CCCC5=CC=CC=C52
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
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.
In vitro activity:
PCS1055 inhibited radioligand [(3)H]-NMS binding to the M4 receptor with a Ki=6.5nM. These GTP-γ-[(35)S] binding studies showed that PCS1055 exhibited 255-, 69.1-, 342- and >1000-fold greater inhibition of Oxo-M activity at the M4 versus the M1-, M2(-), M3-or M5 receptor subtypes, respectively. Schild analyses indicates that PCS1055 acts as a competitive antagonist to muscarinic M4 receptor, and confirms the affinity of the ligand to be low nanomolar, Kb=5.72nM. Reference: Eur J Pharmacol. 2016 Jul 5;782:70-6. https://pubmed.ncbi.nlm.nih.gov/27085897/
In vivo activity:
TBD

Preparing Stock Solutions

The following data is based on the product molecular weight 485.50 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
Croy CH, Chan WY, Castetter AM, Watt ML, Quets AT, Felder CC. Characterization of PCS1055, a novel muscarinic M4 receptor antagonist. Eur J Pharmacol. 2016 Jul 5;782:70-6. doi: 10.1016/j.ejphar.2016.04.022. Epub 2016 Apr 13. PMID: 27085897.
In vitro protocol:
Croy CH, Chan WY, Castetter AM, Watt ML, Quets AT, Felder CC. Characterization of PCS1055, a novel muscarinic M4 receptor antagonist. Eur J Pharmacol. 2016 Jul 5;782:70-6. doi: 10.1016/j.ejphar.2016.04.022. Epub 2016 Apr 13. PMID: 27085897.
In vivo protocol:
TBD
1: Croy CH, Chan WY, Castetter AM, Watt ML, Quets AT, Felder CC. Characterization of PCS1055, a novel muscarinic M4 receptor antagonist. Eur J Pharmacol. 2016 Jul 5;782:70-6. doi:10.1016/j.ejphar.2016.04.022. Epub 2016 Apr 13. PubMed PMID:27085897.