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Dasotraline hydrochloride

Catalog No. T3526   CAS 675126-08-6
Synonyms: SEP-225289 hydrochloride

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

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Dasotraline hydrochloride Chemical Structure
Dasotraline hydrochloride, CAS 675126-08-6
Pack Size Availability Price/USD Quantity
5 mg In stock $ 41.00
10 mg In stock $ 66.00
25 mg In stock $ 98.00
50 mg In stock $ 148.00
1 mL * 10 mM (in DMSO) In stock $ 45.00
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Purity: 99.6%
Purity: 98.92%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Dasotraline hydrochloride (SEP-225289 hydrochloride) (SEP-225289 hydrochloride) is a triple reuptake inhibitor that inhibits dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
Targets&IC50 norepinephrine:6nM, dopamine:4nM, erotonin transporters:11 nM
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 because 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. Average 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].
Synonyms SEP-225289 hydrochloride
Molecular Weight 328.66
Formula C16H16Cl3N
CAS No. 675126-08-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 31 mg/mL (94.32 mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Compound Library Target-Focused Phenotypic Screening Library Clinical Compound Library Bioactive Compounds Library Max Angiogenesis related Compound Library Anti-Obesity Compound Library Neurotransmitter Receptor Compound Library

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Keywords

Dasotraline hydrochloride 675126-08-6 GPCR/G Protein Neuroscience Dopamine Receptor Serotonin Transporter 5-HT Receptor Norepinephrine Dasotraline Dopamine Transporter inhibit Dasotraline Hydrochloride Inhibitor SERT SEP-225289 SEP 225289 Hydrochloride SEP225289 Hydrochloride SLC6A4 SEP 225289 5-HTT DAT SEP225289 SLC6A3 SEP-225289 hydrochloride SEP-225289 Hydrochloride inhibitor

 

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