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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | 6-8 weeks | |
50 mg | $1,980 | 6-8 weeks | |
100 mg | $2,500 | 6-8 weeks |
Description | PCS1055 dihydrochloride is an effective, selective, and competitive muscarinic M4 receptor antagonist (IC50: 18.1 nM and a Kd: 5.72 nM). PCS1055 dihydrochloride is also a potent AChE inhibitor (IC50 s: 22 nM and 120 nM for electric eel and human AChE, res |
In vitro | PCS1055 effectively inhibits G protein activation in a concentration-dependent manner, demonstrating its highest potency at M4 receptors. Research indicates that PCS1055 shows a pronounced binding and functional preference for the M4 receptor subtype, surpassing its affinity and effectiveness for M1-, M2-, M3-, and M5 receptors by 130-, 31.2-, 426-, and >1000-fold, and 255-, 69.1-, 342-, and >1000-fold, respectively. Furthermore, PCS1055 counteracts functional signal transduction, evidenced by its ability to inhibit agonist-stimulated GTP-γ-[35S] binding, showcasing its antagonistic properties. |
In vivo | PCS1055 (30 mg/kg; intraperitoneal injection; male mice) treatment displays the maximal plasma levels at the 30 min time-point with 45100 nM total and 631nM unbound plasma concentrations. At 1 h, the maximal compound exposure observed in the brain is 11.8 nM [1]. |
Molecular Weight | 485.49 |
Formula | C27H34Cl2N4 |
Cas No. | 361979-40-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
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