PCS1055 dihydrochloride

Name: PCS1055 dihydrochloride
Brand: TargetMol
SKU: T16443
Price: 315 USD
Availability: InStock
Rating: 4.5 (1 reviews)

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产品编号 T16443Cas号 361979-40-0

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, respectively). PCS1055 dihydrochloride inhibits radioligand [3H]-NMS binding to the M4 receptor (Ki: 6.5 nM). PCS1055 dihydrochloride shows >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor.

PCS1055 dihydrochloride

还可以

产品编号 T16443Cas号 361979-40-0

规格	价格	库存
25 mg	¥ 10,600	6-8周
50 mg	¥ 13,800	6-8周
100 mg	¥ 17,500	6-8周

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生物活性

产品描述	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, respectively). PCS1055 dihydrochloride inhibits radioligand [3H]-NMS binding to the M4 receptor (Ki: 6.5 nM). PCS1055 dihydrochloride shows >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor.
靶点活性	M4 mAChR:（kd）5.72 nM, M4 mAChR:18.1 nM
体外活性	PCS1055 inhibits G protein activation in a concentration-dependent manner, with the highest potency at the M4 receptors. Both studies show 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 also antagonized functional signal transduction as demonstrates by the inhibition of agonist-stimulated GTP-γ-[35S] binding [1].
体内活性	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].