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Nelotanserin (APD125) 是5-HT2A 强完全逆向激动剂,5-HT2C 中等强度的部分反向激动剂和5-HT2B 的弱反向激动剂,IC50s 值分别为 1.7、79 和 791 nM。
别名 APD125, 1-[3-(4-溴-1-甲基-1H-吡唑-5-基)-4-甲氧基苯基]-3-(2,4-二氟苯基)脲
Nelotanserin (APD125) 是5-HT2A 强完全逆向激动剂,5-HT2C 中等强度的部分反向激动剂和5-HT2B 的弱反向激动剂,IC50s 值分别为 1.7、79 和 791 nM。


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| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 347 | 现货 | |
| 5 mg | ¥ 828 | 现货 | |
| 10 mg | ¥ 1,230 | 现货 | |
| 25 mg | ¥ 1,980 | 现货 | |
| 50 mg | ¥ 3,430 | 现货 | |
| 100 mg | ¥ 4,880 | 现货 | |
| 200 mg | ¥ 6,790 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 796 | 现货 |
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| 产品描述 | Nelotanserin (APD125) is a potent 5-HT2A inverse agonist(IC50 : 1.7 nM), a moderately potent 5-HT2C partial inverse agonist t(IC50 :79 nM )and a weak 5-HT2B inverse agonistt(IC50 : 791 nM). |
| 靶点活性 | 5-HT2B receptor:791 nM, 5-HT2A receptor:1.7 nM, 5-HT2C receptor:79 nM |
| 体内活性 | In healthy human volunteers, nelotanserin was rapidly absorbed after oral administration and achieved maximum concentrations 1 h later. EEG effects occurred within 2 to 4 h after dosing, and were consistent with vigilance-lowering. A dose response of nelotanserin was assessed in a postnap insomnia model in healthy subjects. All doses (up to 40 mg) of nelotanserin significantly improved measures of sleep consolidation, including decreases in the number of stage shifts, number of awakenings after sleep onset, microarousal index, and number of sleep bouts, concomitant with increases in sleep bout duration. Nelotanserin did not affect total sleep time, or sleep onset latency. Furthermore, subjective pharmacodynamic effects observed the morning after dosing were minimal and had no functional consequences on psychomotor skills or memory[1]. |
| 别名 | APD125, 1-[3-(4-溴-1-甲基-1H-吡唑-5-基)-4-甲氧基苯基]-3-(2,4-二氟苯基)脲 |
| 分子量 | 437.24 |
| 分子式 | C18H15BrF2N4O2 |
| CAS No. | 839713-36-9 |
| Smiles | COc1ccc(NC(=O)Nc2ccc(F)cc2F)cc1-c1c(Br)cnn1C |
| 密度 | 1.55 g/cm3 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准 | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 250 mg/mL (571.77 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
该溶液配制表仅适用于固体产品。对于液体产品,请根据标明的浓度或密度计算稀释方案。 | ||||||||||||||||||||||||||||||||||||
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