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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
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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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, SERT:11 nM
In vivo	Acute administration of dasotraline decreases the spontaneous firing rate of LC NE (norepinephrine), VTA DA (dopamine), and DR 5-HT (serotonin) neurons in a dose-dependent manner by activating α2, D2, and 5-HT1A autoreceptors, respectively. Primarily, dasotraline significantly reduces the firing rate of LC NE neurons, while moderately impacting VTA DA and DR 5-HT neuronal activity. Concurrently, SEP-225289, known as (dasotraline), demonstrates equal potency in inhibiting both 5-HT and NE transporters, effectively extending the time for a 50% recuperation of firing activity in dorsal hippocampus CA3 pyramidal neurons following the inhibition induced by the microiontophoretic application of 5-HT and NE. Moreover, the average occupancies of dopamine and serotonin transporters by SEP-225289 escalate with dose increments, showing transporter occupancies of approximately 33%±11% and 2%±13% for 8 mg, 44%±4% and 9%±10% for 12 mg, and 49%±7% and 14%±15% for 16 mg, for dopamine and serotonin transporters, respectively.

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)

References 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-Neurodegenerative Disease Compound Library GPCR Compound Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Drug Library Bioactive Compounds Library Max Target-Focused Phenotypic Screening Library Clinical Compound Library NO PAINS Compound Library

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Keywords

Dasotraline hydrochloride 675126-08-6 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor Serotonin Transporter 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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