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Dasotraline

(Synonyms: SEP 225289)

Dasotraline 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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CAS No.: 675126-05-3
Formula: C₁₆H₁₅Cl₂N
Molecular Weight:292.20

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

Dasotraline Chemical Structure

CAS No.: 675126-05-3

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Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

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

IC₅₀ & Target

IC50: 4 nM (dopamine transporter), 6 nM (norepinephrine transporter),11 nM (5-HT transporter)^[1]

In Vivo

The present in-vivoelectrophysiological study is undertaken to determine the effects of the triple reuptake inhibitor Dasotraline (SEP-225289) on the neuronal activities of locus coeruleus (LC) NE, ventral tegmental area (VTA) DA and dorsal raphe (DR) 5-HT neurons. Administered acutely, 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-HT_1A 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. Dasotraline is equipotent at inhibiting 5-HT and NE transporters since it prolongs to the same extent the time required for a 50% recovery (RT₅₀) of the firing activity of dorsal hippocampus CA3 pyramidal neurons from the inhibition induced by microiontophoretic application of 5-HT and NE. The recovery time (RT), from the suppression of hippocampus pyramidal neuron firing activity following microiontophoresis application of 5-HT and NE, is assessed by determining the RT₅₀ values before and after the acute intravenous administration of cumulative doses of Dasotraline (1–8 mg/kg). Although Dasotraline (1 and 2 mg/kg) does not modify the firing activity of CA3 pyramidal neurons, a significant reduction (∼50%) is detected with the highest dose (8 mg/kg). In rats pre-treated with WAY100635, Dasotraline (0.5-2 mg/kg i.v.) elicits a significant increase in DR 5-HT firing rate. In rats pre-treated with WAY100635, Dasotralinesignificantly increases the number of single spikes and bursts^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 675126-05-3
Molecular Weight 292.20
Formula C₁₆H₁₅Cl₂N
SMILES

N[C@@H]1CC[C@@H](C2=CC=C(Cl)C(Cl)=C2)C3=CC=CC=C31
Synonyms

SEP 225289
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : ≥ 31 mg/mL (106.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.4223 mL

17.1116 mL

34.2231 mL

5 mM

0.6845 mL

3.4223 mL

6.8446 mL

10 mM

0.3422 mL

1.7112 mL

3.4223 mL

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight

Dilution Calculator

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
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g
Dosing Volume (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.4223 mL	17.1116 mL	34.2231 mL	85.5578 mL
	5 mM	0.6845 mL	3.4223 mL	6.8446 mL	17.1116 mL
	10 mM	0.3422 mL	1.7112 mL	3.4223 mL	8.5558 mL
	15 mM	0.2282 mL	1.1408 mL	2.2815 mL	5.7039 mL
	20 mM	0.1711 mL	0.8556 mL	1.7112 mL	4.2779 mL
	25 mM	0.1369 mL	0.6845 mL	1.3689 mL	3.4223 mL
	30 mM	0.1141 mL	0.5704 mL	1.1408 mL	2.8519 mL
	40 mM	0.0856 mL	0.4278 mL	0.8556 mL	2.1389 mL
	50 mM	0.0684 mL	0.3422 mL	0.6845 mL	1.7112 mL
	60 mM	0.0570 mL	0.2852 mL	0.5704 mL	1.4260 mL
	80 mM	0.0428 mL	0.2139 mL	0.4278 mL	1.0695 mL
	100 mM	0.0342 mL	0.1711 mL	0.3422 mL	0.8556 mL

Keywords

100 mg

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Biological Activity
- Description
- IC50 & Target
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo Dissolution Calculator
Purity & Documentation
References

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Dasotraline

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Dasotraline Related Classifications

Cat. No.: HY-12850