PCS1055 dihydrochloride
Modify Date: 2025-08-23 17:59:53
PCS1055 dihydrochloride structure
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Common Name | PCS1055 dihydrochloride | ||
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| CAS Number | 361979-40-0 | Molecular Weight | 485.49 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C27H34Cl2N4 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of PCS1055 dihydrochloridePCS1055 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[1][2]. |
| Name | PCS1055 dihydrochloride |
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| 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[1][2]. |
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| Related Catalog | |
| Target |
IC50: 18.1 nM (Muscarinic M4 receptor); Kd: 5.72 nM (Muscarinic M4 receptor)[1]; IC50: 22 nM (Electric eel AChE) and 120 nM (Human AChE)[2] |
| 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[1]. |
| 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[1]. Animal Model: Male mice[1] Dosage: 30 mg/kg Administration: Intraperitoneal injection (Pharmacokinetic Analysis) Result: The maximal plasma levels were observed at the 30 min time-point with 45100 nM total and 631nM unbound plasma concentrations. The maximal compound exposure observed in the brain was 11.8 nM at 1 h. |
| References |
| Molecular Formula | C27H34Cl2N4 |
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| Molecular Weight | 485.49 |