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品質等級
化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
white to beige
溶解度
H2O: 5 mg/mL, clear (warmed)
儲存溫度
2-8°C
SMILES 字串
[H]Cl.[H]Cl.C12=C(N=NC(NCCC3CCN(CC4=CC=CC=C4)CC3)=C2)C5=C(C=CC=C5)CCC1
生化/生理作用
PCS1055 是高效的、选择性毒蕈碱型 M4 乙酰胆碱受体竞争性拮抗剂,比对 M1、M3 和 M5 受体的选择性 > 100 倍,比对 M2 受体的选择性高 30 倍。PCS1055 最初被描述为高效电鳗 AChE 抑制剂(IC50 = 22 nM),而对人 AChE 的效力较弱(IC50 = 120 nM)。
European journal of pharmacology, 782, 70-76 (2016-04-18)
Identification of synthetic ligands selective for muscarinic receptor subtypes has been challenging due to the high sequence identity and structural homology among the five muscarinic acetylcholine receptors. Here, we report the pharmacological characterization of PCS1055, a novel muscarinic M4 receptor
Journal of medicinal chemistry, 44(17), 2707-2718 (2001-08-10)
Starting from the 3-[2-(1-benzylpiperidin-4-yl)ethylamino]-6-phenylpyridazine 1, we performed the design, the synthesis, and the structure-activity relationships of a series of pyridazine analogues acting as AChE inhibitors. Structural modifications were achieved on four different parts of compound 1 and led to the
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