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Tianeptine metabolite MC5是一种来自非典型抗抑郁化合物tianeptine的活性代谢物,通过β-氧化形成。此代谢物在使用表达人类μ-阿片受体(MOR)而非人类δ-阿片受体(DOR;EC50s = 0.454和 >100 µM, 分别)的HEK293T细胞进行的生物发光共振能量转移(BRET)试验中,特异性诱导G蛋白激活。在野生型小鼠上,30 mg/kg剂量的Tianeptine metabolite MC5可减少强迫游泳测试中的静止时间,但在MOR敲除小鼠中则不会,表明其具有MOR依赖的抗抑郁样活性。
Tianeptine metabolite MC5是一种来自非典型抗抑郁化合物tianeptine的活性代谢物,通过β-氧化形成。此代谢物在使用表达人类μ-阿片受体(MOR)而非人类δ-阿片受体(DOR;EC50s = 0.454和 >100 µM, 分别)的HEK293T细胞进行的生物发光共振能量转移(BRET)试验中,特异性诱导G蛋白激活。在野生型小鼠上,30 mg/kg剂量的Tianeptine metabolite MC5可减少强迫游泳测试中的静止时间,但在MOR敲除小鼠中则不会,表明其具有MOR依赖的抗抑郁样活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 3,550 | 35日内发货 | |
5 mg | ¥ 16,800 | 35日内发货 | |
10 mg | ¥ 26,600 | 35日内发货 |
产品描述 | Tianeptine metabolite MC5, an active derivative of the atypical antidepressant tianeptine produced through β-oxidation, exhibits selective G protein activation in bioluminescence resonance energy transfer (BRET) assays. Utilizing HEK293T cells expressing the human μ-opioid receptor (MOR) over the human δ-opioid receptor (DOR; EC50s = 0.454 and >100 µM, respectively), it demonstrates specificity. Moreover, this metabolite reduces immobility in wild-type mice during the forced swim test at a dose of 30 mg/kg, an effect not observed in MOR knockout mice, suggesting its antidepressant-like activity is MOR-dependent. |
分子量 | 430.88 |
分子式 | C19H20ClN2O4S.Na |
CAS No. | 115220-11-6 |
存储 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | Ethanol: Slightly soluble Methanol: Slightly soluble DMSO: Slightly soluble Dichloromethane: Slightly soluble |
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