2614W94 - CAS:205187-35-5 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	2614W94
英文名称:	2614W94
别名:	3-(1,1,1-trifluoropropan-2-yloxy)phenoxathiine 10,10-dioxide
CAS No:	205187-35-5	分子式:	C₁₅H₁₁F₃O₄S	分子量:	344.31
CAS No:	205187-35-5
分子式:	C₁₅H₁₁F₃O₄S
分子量:	344.31

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W10062 2614W94 (psaitong)

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包装规格：

1g in glass bottle

产品描述：

基本信息

产品编号：	W10062
产品名称：	2614W94
CAS:	205187-35-5	储存条件	粉末	-20℃	四年

分子式：	C15H11F3O4S		溶于液体
分子量	344.31
化学名：	3-(1,1,1-trifluoropropan-2-yloxy)phenoxathiine 10,10-dioxide
Solubility (25°C)：
体外:	DMSO
	Ethanol
	Water
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

生物活性

产品描述	具有选择性的，可逆的monoamine oxidase-A抑制剂，IC50值和Ki值分别为5nM和1.6nM。
靶点	IC50: 5nM (Monoamine Oxidase) Ki: 1.6nM (Monoamine Oxidase)
体外研究	2614W94 shows potent inhibitory activity against MAO-A, but shows no inhibition of MAO-B at 30nM
体内研究	2614W94 (5 mg/kg, p.o.) produces selective inhibition of MAO-A in brains and livers of rats. 2614W94 (5 mg/kg, p.o.) also causes an elevation of neurotransmitter amines in brain, inparticular serotonin and norepinephrine, with a concomitant decrease in their oxidized metabolites. 2614W94 (0.5, 1, 2 mg/kg, p.o.) potentiates 5-hydroxytryptophan-induced head twitches in rats in a dose-dependent manner, with an extrapolated ED50 of 1.1 mg/kg.

推荐实验方法(仅供参考)

Kinase Assay

MAO-A and -B forms are assayed. Rat brain mito-chondrial extract is pre-incubated with the inhibitor for 15 min at 37°C in 50mM potassium phosphate buffer (pH 7.4). Substrates [3H]serotonin (0.2mM, 5 Ci/mol) and [14C]β-phene-thylamine (10 µM, 3 Ci/mol) are then added, and incubation at 37°C is continued for 20 min. Blank assays contain 2mM pargyline to inhibit all MAO activity. The reaction is terminated with 0.2 mL of 2 N HCl, and products are extracted with 6mL of ethyl acetate/toluene (1:1). A 4mL aliquot of the organic layer is countedin 10mL of Ecolite in a scintillation spectrometer programmed for double-label counting. Assays are performed in triplicate unless otherwise indicated. At the above concentrations, serotonin is a selective substrate for MAO-A, and β-phenethylamine is aselective substrate for MAO-B.

Animal Administration

Rats: Nonfasted Sprague-Dawley male rats (250-350 g) are dosed by gavage with 0.5% methyl cellulose or with 2614W94 or other compounds suspended in the methyl cellulose vehicle. For all groups, n = 3 unless otherwise specified. For oral administration, dosing volume is 10 mL/kg of body weight. For intravenous dosing, the vehicle is a mixture of PEG 400 (polyethylene glycol; molecular weight, 400), ethanol, and physiologic saline in a volume ratio of 1.5/1.5/1.0, respectively, and the dosing volume is 1mL/kg. After dosing, rats are returned to their cages and allowed free access to water. Any animals kept overnight are also given food. Death is by CO2 asphyxiation, after which brains and livers are promptly removed, frozen on dry ice, and stored at -70°C.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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