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Flumexadol

Flumexadol

产品编号 T11302   CAS 30914-89-7

Flumexadol is a selective and affinity 5-HT2C receptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2A receptor. Flumexadol is an orally active non-narcotic analgesic.

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Flumexadol Chemical Structure
Flumexadol, CAS 30914-89-7
规格 价格/CNY 货期 数量
2 mg ¥ 643 5日内发货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Flumexadol (T11302)
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参考文献
产品描述 Flumexadol is a selective and affinity 5-HT2C receptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2A receptor. Flumexadol is an orally active non-narcotic analgesic.
靶点活性 5-HT2C receptor:25 nM (ki)
体内活性 In rats and dogs dosed with 14C-Flumexadol (CERM1841), the 14C is excreted in the urine.?The 14C 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.
分子量 231.21
分子式 C11H12F3NO
CAS No. 30914-89-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (432.51 mM), Sonication is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.3251 mL 21.6254 mL 43.2507 mL 108.1268 mL
5 mM 0.865 mL 4.3251 mL 8.6501 mL 21.6254 mL
10 mM 0.4325 mL 2.1625 mL 4.3251 mL 10.8127 mL
20 mM 0.2163 mL 1.0813 mL 2.1625 mL 5.4063 mL
50 mM 0.0865 mL 0.4325 mL 0.865 mL 2.1625 mL
100 mM 0.0433 mL 0.2163 mL 0.4325 mL 1.0813 mL

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TargetMol Library Books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)tetrahydro-1,4-oxazine (CERM) 1841) in rats and dogs. Xenobiotica. 1979 Nov;9(11):703-11.
WAY 163909 3-Hydroxy agomelatine D3 Phenylbiguanide Rodatristat ethyl Geissoschizine methyl ether N-Desmethylclozapine Befiradol hydrochloride ATC 0175 hydrochloride

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Keywords

Flumexadol 30914-89-7 GPCR/G Protein Neuroscience 5-HT Receptor Inhibitor inhibitor inhibit

 

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