Flumexadol

目录号: PL09163 纯度: ≥98%
Flumexadol 是一种选择性和亲和力的 5-HT2C 受体激动剂,对于 Flumexadol 的 (+)-对映体,Ki 为 25 nM,选择性是 5-HT2A 受体的 40 倍。Flumexadol 是一种具有口服活性,可用于缓解疼痛的研究的化合物。
CAS No. :30914-89-7
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中文名称
Flumexadol
中文别名
氟甲沙朵
英文名称
Flumexadol
英文别名
Morpholine,2-[3-(trifluoromethyl)phenyl]-;1841CERM;2-(3-(Trifluoromethyl)phenyl)morpholine;2-(3-Trifluormethylphenyl)-1,4-tetrahydro-oxazin;2-(3-trifluoromethyl-phenyl)-morpholine;2-< 3-(Trifluormethyl)-phenyl> -tetrahydro-1,4-oxazin;BRN 1215543;CERM-1841;Flumexadol;Flumexadolum [INN-Latin]
Cas No.
30914-89-7
分子式
C11H12NOF3
分子量
231.21
包装储存
Pure form -20°C 3 years;4°C 2 years
详情描述
Flumexadol 是一种选择性和亲和力的 5-HT2C 受体激动剂,对于 Flumexadol 的 (+)-对映体,Ki 为 25 nM,选择性是 5-HT2A 受体的 40 倍。Flumexadol 是一种具有口服活性,可用于缓解疼痛的研究的化合物。
产品详情
Flumexadol 是一种选择性和亲和力的 5-HT2C 受体激动剂,对于 Flumexadol 的 (+)-对映体,Ki 为 25 nM,选择性是 5-HT2A 受体的 40 倍。Flumexadol 是一种具有口服活性,可用于缓解疼痛的研究的化合物。
生物活性
Flumexadol is a selective and affinity 5-HT 2C receptor agonist with a K i of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT 2A receptor. Flumexadol is an orally active non-narcotic analgesic.
性状
Liquid
IC50 & Target[1][2]
5-HT2C Receptor 25 nM (Ki)
体内研究(In Vivo)
In rats and dogs dosed with C-Flumexadol (CERM1841), the C is excreted in the urine. The C eliminated in the faeces of dog is significantly higher than for rat. Conjugated metabolites, mostly glucuronides, accounted for the greater part of the urinary radioactivity in both species. Biotransformation products are predominantly acids in both species, follows by significant amounts of basic metabolites, with very little neutral substances. The major urinary metabolite in rats is 3-trifluoromethylbenzoic acid and 3-trifluoromethylhipuric acid. In the dog it is 3-trifluoromethylmandelic acid in addition to the benzoic acid and its conjugate. The basic products identified in the urine of both species are unchanged drug and 1-amino-2-hydroxy-2-(3-trifluoromethylphenyl)ethane, with the first predominating. has not independently
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years;4°C 2 years
参考文献
[1]. Hache J, et al. The pharmacology of 1841 CERM, a new analgesic. Arzneimittelforschung. 1978;28(4):642-5.
[2]. Nilsson BM. 5-Hydroxytryptamine 2C (5-HT2C) receptor agonists as potential antiobesity agents. J Med Chem. 2006 Jul 13;49(14):4023-34.
[3]. Kucharczyk N, et al. Metabolites of 2-(3-trifluoromethylphenyl
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (144.15 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Hache J, et al. The pharmacology of 1841 CERM, a new analgesic. Arzneimittelforschung. 1978;28(4):642-5.
[2]. Nilsson BM. 5-Hydroxytryptamine 2C (5-HT2C) receptor agonists as potential antiobesity agents. J Med Chem. 2006 Jul 13;49(14):4023-34.
[3]. Kucharczyk N, et al. Metabolites of 2-(3-trifluoromethylphenyl

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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