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Dasotraline hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dasotraline hydrochloride图片
CAS NO:675126-08-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
SEP-225289 hydrochloride
产品介绍
Dasotraline hydrochloride (SEP-225289 hydrochloride) 是具有阻断多巴胺,去甲肾上腺素和三羟色胺转运蛋白的三重再摄取抑制剂,IC50值分别为4,6和11 nM。
生物活性

Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocksdopamine,norepinephrine, andserotonintransporters withIC50values of 4, 6, and 11 nM, respectively.

IC50& Target

IC50: 4 nM (dopamine), 6 nM (norepinephrine), 11 nM (serotonin)[1]

体内研究
(In Vivo)

Acute administration of dasotraline dose-dependently decreases the spontaneous firing rate of LC NE, VTA DA and DR 5-HT neurons through the activation of α2, D2 and 5-HT1A autoreceptors, respectively. Dasotraline predominantly inhibits the firing rate of LC NE neurons while producing only a partial decrease in VTA DA and DR 5-HT neuronal discharge. SEP-225289 is equipotent at inhibiting 5-HT and NE transporters since it prolongs to the same extent the time required for a 50% recovery of the firing activity of dorsal hippocampus CA3 pyramidal neurons from the inhibition induced by microiontophoretic application of 5-HT and NE[1]. Average dopamine and serotonin transporter occupancies increase with increasing doses of SEP-225289. Mean dopamine and serotonin transporter occupancies are 33%±11% and 2%±13%, respectively, for 8 mg; 44%±4% and 9%±10%, respectively, for 12 mg; and 49%±7% and 14%±15%, respectively, for 16 mg[2].

Clinical Trial
分子量

328.66

性状

Solid

Formula

C16H16Cl3N

CAS 号

675126-08-6

中文名称

达索曲林盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 31 mg/mL(94.32 mM)

H2O : 1.61 mg/mL(4.90 mM;ultrasonic and warming and heat to 60℃)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.0427 mL15.2133 mL30.4266 mL
5 mM0.6085 mL3.0427 mL6.0853 mL
10 mM0.3043 mL1.5213 mL3.0427 mL
*

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
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。