2. Neuronal Signaling
  3. Serotonin Transporter Dopamine Transporter
  4. Dasotraline hydrochloride

Dasotraline hydrochloride  (Synonyms: SEP-225289 hydrochloride)

Cat. No.: HY-12850A Purity: 99.74%
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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

Dasotraline hydrochloride Chemical Structure

CAS No. : 675126-08-6

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Based on 1 publication(s) in Google Scholar

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Description

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.

IC50 & Target

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

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

328.66

Formula

C16H16Cl3N
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (94.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.0427 mL 15.2133 mL 30.4266 mL 76.0665 mL
DMSO 5 mM 0.6085 mL 3.0427 mL 6.0853 mL 15.2133 mL
10 mM 0.3043 mL 1.5213 mL 3.0427 mL 7.6066 mL
15 mM 0.2028 mL 1.0142 mL 2.0284 mL 5.0711 mL
20 mM 0.1521 mL 0.7607 mL 1.5213 mL 3.8033 mL
25 mM 0.1217 mL 0.6085 mL 1.2171 mL 3.0427 mL
30 mM 0.1014 mL 0.5071 mL 1.0142 mL 2.5355 mL
40 mM 0.0761 mL 0.3803 mL 0.7607 mL 1.9017 mL
50 mM 0.0609 mL 0.3043 mL 0.6085 mL 1.5213 mL
60 mM 0.0507 mL 0.2536 mL 0.5071 mL 1.2678 mL
80 mM 0.0380 mL 0.1902 mL 0.3803 mL 0.9508 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dasotraline675126-08-6SEP-225289SEP225289SEP 225289Serotonin TransporterDopamine Transporter5-HTTSERTSLC6A4DATSLC6A3Inhibitorinhibitorinhibit

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