Flumexadol,98.87%
产品编号:Bellancom-133024| CAS NO:30914-89-7| 分子式:C11H12F3NO| 分子量:231.21
Flumexadol 是一种口服活性非麻醉镇痛药。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。
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Flumexadol
产品介绍 | 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。 | ||||||||||||||||
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生物活性 | 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. | ||||||||||||||||
体外研究 | |||||||||||||||||
体内研究 |
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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
体内研究 |
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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
性状 | Liquid | ||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : 33.33 mg/mL (144.15 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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参考文献 |
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海关编码 | 2934999090 |
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~% ![]() 30914-89-7 |
文献:Busch,N. et al. European Journal of Medicinal Chemistry, 1976 , vol. 11, p. 201 - 207 |
~% ![]() 30914-89-7 |
文献:Busch,N. et al. European Journal of Medicinal Chemistry, 1976 , vol. 11, p. 201 - 207 |
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