Roluperidone-CYR-101-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERoluperidoneCat. No.: HY-19469CAS No.: 359625-79-9Synonyms: CYR-101; MIN-101; MT-210分式: CHFNO分量: 366.43作靶点: 5-HT Receptor; Sigma Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6

2、months-20C 1 month溶解性数据体外实验 DMSO : 33.33 mg/mL (90.96 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 3 mg/mL (8.19 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 3 mg/mL (8.19 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL AC

3、TIVITY物活性 Roluperidone (CYR-101)种新型环酰胺衍物，对 5-HT2A 和 sigma-2 受体具有亲和，Ki 分别为 7.53nM 和 8.19 nM。IC50 & Target Ki: 7.53 nM (5-HT2A), 8.19 nM (sigma-2) 1体外研究 Roluperidone (CYR-101) also shows binding affinity for 1-adrenergic receptors but low or no affinity formuscarinic, cholinergic, and histaminergic re

4、ceptors. Although Roluperidone (CYR-101) has no affinities forpre- or postsynaptic dopaminergic receptors, it is probable that sigma-2 receptors are implicated in themodulation of dopamine and glutamatergic pathways, as well as in calcium neuronal modulation 1.REFERENCES1. Davidson M, et al. Efficac

5、y and Safety of MIN-101: A 12-Week Randomized, Double-Blind, Placebo-Controlled Trial of a New Drug inDevelopment for the Treatment of Negative Symptoms in Schizophrenia. Am J Psychiatry. 2017 Jul 28:appiajp201717010122.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 021-589