产品
编 号：F336410
分子式：C27H34Cl2N4
分子量：485.49
分子式：C27H34Cl2N4
分子量：485.49
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 361979-40-0
产品详情
生物活性：
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.
体内研究：
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.Animal Model:Male mice
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.
体外研究：
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.
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.
体内研究：
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.Animal Model:Male mice
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.
体外研究：
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.
产品资料
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