Fig. 1 · Structure
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PCS1055 dihydrochloride
M4 Receptor Antagonist
PCS1055 dihydrochloride is a selective and competitive antagonist of the muscarinic M4 receptor, with an IC50 value of 18.1 nM and a Kd of 5.72 nM. This compound effectively inhibits the binding of the radioligand [3H]-NMS to the M4 receptor, displaying a Ki of 6.5 nM. PCS1055 dihydrochloride demonstrates over 100-fold selectivity against M1, M3, and M5 receptors, and 30-fold selectivity at the M2 receptor. Additionally, it serves as a potent acetylcholinesterase inhibitor, with IC50 values of 22 nM and 120 nM for electric eel and human AChE, respectively, highlighting its potential for various neurological research applications.
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Specifications
| Manufacturer | Adooq Bioscience |
|---|---|
| Actions | Antagonist |
| CAS Number | 361979-40-0 |
| Applications | M4 Receptor Antagonist |
| Formula | C27H34Cl2N4 |
| Molecular Weight | 485.49 |
| SMILES | [H]Cl.[H]Cl.C12=NN=C(NCCC3CCN(CC4=CC=CC=C4)CC3)C=C1CCCC5=CC=CC=C52 |
Storage & Solubility
In Vitro Solubility
Reported Solubility
No reported solubility data are available for this product.
Preparing Stock Solutions
| Concentration | |
|---|---|
Values use four significant digits. Prepare to the final solution volume; this is not the volume of solvent to add.
Stock preparation is unavailable for this product molecular weight.
Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.
Storage
Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.