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Ansofaxine hydrochloride (LY03005) 是一种血清素-去甲肾上腺素-多巴胺再摄取抑制剂,IC50值分别为723、491 和 763 nM。
Ansofaxine hydrochloride (LY03005) 是一种血清素-去甲肾上腺素-多巴胺再摄取抑制剂,IC50值分别为723、491 和 763 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 528 | 现货 | |
5 mg | ¥ 1,230 | 现货 | |
10 mg | ¥ 1,990 | 现货 | |
25 mg | ¥ 3,580 | 现货 | |
50 mg | ¥ 5,130 | 现货 | |
100 mg | ¥ 7,170 | 现货 | |
500 mg | ¥ 14,300 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,360 | 现货 |
产品描述 | Ansofaxine hydrochloride (LY03005) is a serotonin-norepinephrine-dopamine reuptake inhibitor (IC50s: 723, 763 and 491 nM, respectively). |
靶点活性 | Dopamine:491 nM, Norepinephrine:763 nM, 5-HT:723 nM |
体内活性 | 通过口服溶液(0.06 mmol/kg p.o.)、口服悬浮液(0.06 mmol/kg p.o.)和静脉注射溶液(0.04 mmol/kg i.v.)急性给药,对啮齿动物施用Ansofaxine和desvenlafaxine。同时,两种药物的口服悬浮液(0.06 mmol/kg/天)也被用于14天的慢性期给药。Ansofaxine快速渗透至大鼠纹状体,转化为desvenlafaxine并展示了相较于单独给予desvenlafaxine时更大的总体曝光量。Ansofaxine的急性及慢性口服悬浮液给药,相比于desvenlafaxine的相应给药,更能增加5-HT、DA和NE水平[1]。Ansofaxine的最大耐受剂量(MTD)为500 mg/kg,单次给药的致死剂量为1000 mg/kg,在SD大鼠中。经过13周的重复剂量口服毒性测试,Ansofaxine的未观察到不良效应水平(NOAEL)对于大鼠而言大于300 mg/kg [2]。 |
动物实验 | The dosages of LPM570065 and desvenlafaxine used with different administration routes referred to previous studies and was determined by preliminary experiments. Oral solutions of LPM570065 and desvenlafaxine for intragastric administration (0.06 mmol/kg p.o.) were prepared by dissolving the compounds in 10% glucose. Oral suspensions of LPM570065 and desvenlafaxine for intragastric administration (0.06 mmol/kg p.o.) were prepared by suspending the compounds in 0.5% carboxymethylcellulose sodium. Intravenous solutions of LPM570065 and desvenlafaxine for intravenous administration (0.04 mmol/kg i.v.) were prepared by dissolving the compounds in 10% glucose. WAY-100635 was dissolved in 0.9% saline and was administered subcutaneously (0.3 mg/kg s.c.). Raclopride was dissolved in 0.9% saline and was administered subcutaneously (0.5 mg/kg s.c.). Different vehicles were used for administration using different administration routes [1]. |
别名 | Ansofaxine盐酸盐, LPM570065, LY03005 |
分子量 | 417.97 |
分子式 | C24H32ClNO3 |
CAS No. | 916918-84-8 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | DMSO: 16.67 mg/mL (39.88 mM) | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
DMSO
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