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(S)-5-羟基-6-甲氧基Duloxetine是(S)-duloxetine的一个活性代谢物,主要通过对血清素(5-HT)和去甲肾上腺素的再摄取进行抑制。它通过(S)-duloxetine经过一个5-或6-羟基Duloxetine中间体以及一个儿茶酚Duloxetine中间体形成,这些中间体由细胞色素P450 (CYP)同型酶CYP1A2和CYP2D6形成。(S)-5-羟基-6-甲氧基Duloxetine在脂质膜中抑制5-HT转运体(SERT)、去甲肾上腺素转运体(NET)和多巴胺转运体(DAT),其对人类转运体的抑制常数(Kis)分别为266、920和2,814 nM。
(S)-5-羟基-6-甲氧基Duloxetine是(S)-duloxetine的一个活性代谢物,主要通过对血清素(5-HT)和去甲肾上腺素的再摄取进行抑制。它通过(S)-duloxetine经过一个5-或6-羟基Duloxetine中间体以及一个儿茶酚Duloxetine中间体形成,这些中间体由细胞色素P450 (CYP)同型酶CYP1A2和CYP2D6形成。(S)-5-羟基-6-甲氧基Duloxetine在脂质膜中抑制5-HT转运体(SERT)、去甲肾上腺素转运体(NET)和多巴胺转运体(DAT),其对人类转运体的抑制常数(Kis)分别为266、920和2,814 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 3,220 | 期货 | |
5 mg | ¥ 14,500 | 期货 |
产品描述 | (S)-5-hydroxy-6-methoxy Duloxetine, an active metabolite of the (S)-duloxetine, functions as a serotonin (5-HT) and norepinephrine reuptake inhibitor. Its formation occurs through the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2D6 via a 5- or 6-hydroxy duloxetine intermediate, followed by a catechol duloxetine intermediate. This compound effectively inhibits the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT) across lipid membranes, with inhibition constants (Kis) of 266, 920, and 2,814 nM, respectively, for human transporters. |
分子量 | 459.51 |
分子式 | C19H21NO3S.C4H4O4 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | Methanol: soluble DMF: soluble Ethanol: soluble DMSO: soluble |
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