Roluperidone (Synonyms: CYR-101; MIN-101; MT-210)
目录号: PL11283 纯度: ≥99%
CAS No. :359625-79-9
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中文名称
Roluperidone
中文别名
2-[[1-[2-(4-氟苯基)-2-氧代乙基]-4-哌啶基]甲基]-2,3-二氢-1H-异吲哚-1-酮
英文名称
Roluperidone
英文别名
2-[[1-[2-(4-fluorophenyl)-2-oxoethyl]piperidin-4-yl]methyl]-3H-isoindol-1-one;MIN-101;MT-210;CYR 101;CYR-101;Roluperidone;4P31I0M3BF;2-((1-(2-(4-fluorophenyl)-2-oxoethyl)piperidin-4-yl)methyl)isoindolin-1-one;Roluperidon;Roluperidone (USAN);DB13080;1H-Isoindol-1-one, 2-((1-(2-(4-fluorophenyl)-2-oxoethyl)-4-piperidinyl)methyl)-2,3-dihydro-;D11258;Q25100536
Cas No.
359625-79-9
分子式
C22H23FN2O2
分子量
366.43
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Roluperidone (CYR-101) 是一种新型环酰胺衍生物,对 5-HT2A 和 sigma-2 受体具有高亲和力,Ki 分别为 7.53 nM 和 8.19 nM。
生物活性
Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for 5-HT 2A and sigma-2 receptors (K i of 7.53 nM and 8.19 nM for 5-HT 2A and sigma-2, respectively).
性状
Solid
IC50 & Target[1][2]
5-HT2A Receptor 7.53 nM (Ki) Sigma-2 Receptor
体外研究(In Vitro)
Roluperidone (CYR-101) also shows binding affinity for α1-adrenergic receptors but low or no affinity for muscarinic, cholinergic, and histaminergic receptors. Although Roluperidone (CYR-101) has no affinities for pre- or postsynaptic dopaminergic receptors, it is probable that sigma-2 receptors are implicated in the modulation of dopamine and glutamatergic pathways, as well as in calcium neuronal modulation. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Davidson M, et al. Efficacy and Safety of MIN-101: A 12-Week Randomized, Double-Blind, Placebo-Controlled Trial of a New Drug in Development for the Treatment of Negative Symptoms in Schizophrenia. Am J Psychiatry. 2017 Jul 28:appiajp201717010122.
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (90.96 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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