| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Dasotraline (formerly known as SEP-225289; SEP-225,289) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) with anti-depressant and anti-ADHD activity. The drug is no longer being developed for major depressive disorder (MDD), but is still under investigation for the treatment of attention-deficit hyperactivity disorder (ADHD) and eating disorders.
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| ln Vivo |
Dasotraline administered acutely dose-dependently inhibits the spontaneous firing rate of LC NE, VTA DA, and DR 5-HT neurons via activating their respective α2, D2, and 5-HT1A autoreceptors. Dasotraline only somewhat reduces VTA DA and DR 5-HT neuronal discharge, however it primarily suppresses the firing rate of LC NE neurons. Since SEP-225289 extends the time required for a 50% recovery of the firing activity of dorsal hippocampal CA3 pyramidal neurons from the inhibition generated by microiontophoretic administration of 5-HT and NE, it is equipotent at blocking 5-HT and NE transporters[1]. As SEP-225289 dosage increases, average dopamine and serotonin transporter occupancies rise as well. The average occupancies of dopamine and serotonin transporters are 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, respectively[2].
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| References |
| Molecular Formula |
C16H16CL3N
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|---|---|
| Molecular Weight |
328.6639
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| Exact Mass |
327.034
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| CAS # |
675126-08-6
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| Related CAS # |
Dasotraline;675126-05-3
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| PubChem CID |
25192248
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| Appearance |
White to off-white solid powder
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| LogP |
6.421
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
309
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1C[C@H](C2=CC=CC=C2[C@@H]1C3=CC(=C(C=C3)Cl)Cl)N.Cl
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| InChi Key |
YKXHIERZIRLOLD-DFIJPDEKSA-N
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| InChi Code |
InChI=1S/C16H15Cl2N.ClH/c17-14-7-5-10(9-15(14)18)11-6-8-16(19)13-4-2-1-3-12(11)13/h1-5,7,9,11,16H,6,8,19H21H/t11-,16+/m0./s1
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| Chemical Name |
(1R,4S)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-amine hydrochloride
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| Synonyms |
SEP225289SEP-225,289 DasotralineSEP225,289 SEP225289 Dasotraline HCl SEP225,289 SEP-225289Dasotraline hydrochloride.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 31 mg/mL (~94.32 mM)
H2O : ~1.61 mg/mL (~4.90 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02457819 | Completed | Drug:Dasotraline | Attention Deficit Hyperactivity Disorder | Sumitomo Pharma America,Inc. | June 30, 2015 | Phase 3 |
| NCT02564588 | Completed | Drug:Dasotraline Drug:Placebo |
Binge Eating Disorder | Sumitomo Pharma America,Inc. | October 2015 | Phase 2 Phase 3 |
| NCT03107026 | Completed | Drug:dasotraline 4mg Drug:dasotraline 6mg Drug:Placebo |
Binge Eating Disorder | Sumitomo Pharma America,Inc. | March 31, 2017 | Phase 3 |
| NCT03231800 | Completed | Drug:dasotraline Drug:Placebo |
Attention-Deficit Hyperactivity Disorder(ADHD) |
Sumitomo Pharma America,Inc. | July 31, 2017 | Phase 3 |
| NCT02160262 | Completed | Drug:Dasotraline | Adult Attention Deficit Hyperactivity Disorder |
Sumitomo Pharma America,Inc. | June 2014 | Phase 3 |
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