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Dasotraline hydrochloride

Catalog No.GC19118

Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.

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Dasotraline hydrochloride Chemical Structure

Cas No.: 675126-08-6

Size Price Stock Qty
10mM (in 1mL DMSO)
$33.00
In stock
5mg
$45.00
In stock
10mg
$72.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.

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].

References:
[1]. Guiard BP, et al. Characterization of the electrophysiological properties of triple reuptake inhibitors on monoaminergic neurons. Int J Neuropsychopharmacol. 2011 Mar;14(2):211-23.
[2]. DeLorenzo C, et al. SEP-225289 serotonin and dopamine transporter occupancy: a PET study.

Chemical Properties

Cas No. 675126-08-6 SDF
Canonical SMILES N[C@@H]1CC[C@@H](C2=CC=C(Cl)C(Cl)=C2)C3=CC=CC=C31.Cl[H]
Formula C16H16Cl3N M.Wt 328.66
Solubility DMSO : ≥ 31 mg/mL (94.32 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.0427 mL 15.2133 mL 30.4266 mL
5 mM 0.6085 mL 3.0427 mL 6.0853 mL
10 mM 0.3043 mL 1.5213 mL 3.0427 mL
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