| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
DSP-1053 targets the serotonin transporter (SERT) with high affinity (Ki = 1.02 nM) and also acts as a partial agonist at the 5-HT1A receptor (Ki = 5.05 nM). SERT is responsible for the reuptake of serotonin from the synaptic cleft back into presynaptic neurons, and its inhibition increases synaptic serotonin levels. The 5-HT1A receptor is a G protein-coupled receptor that regulates serotonin release through autoreceptor-mediated negative feedback. By combining SERT inhibition with partial 5-HT1A agonism, DSP-1053 increases serotonin availability while potentially reducing the delayed onset and side effects associated with conventional SSRIs.
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| ln Vitro |
In vitro, DSP-1053 demonstrates potent inhibition of the serotonin transporter with a Ki of 1.02 nM. The compound also shows partial agonistic activity at the 5-HT1A receptor with a Ki of 5.05 nM. The combination of SERT inhibition and 5-HT1A receptor partial agonism makes DSP-1053 a unique pharmacological tool for studying serotonin signaling. The compound exhibits high potency and selectivity for its targets, with minimal off-target activity against other neurotransmitter transporters and receptors. In cellular assays, DSP-1053 effectively inhibits serotonin uptake and modulates 5-HT1A receptor-mediated signaling pathways including G protein activation and downstream cAMP modulation.
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| ln Vivo |
In vivo, DSP-1053 has demonstrated antidepressant-like activity in animal models. The compound significantly enhances memory performance in cognitive tests with a minimum effective dose of 3 mg/kg. In rodent models of depression (e.g., forced swim test, tail suspension test), DSP-1053 reduces immobility time, indicating antidepressant efficacy. The compound also shows anxiolytic-like effects in elevated plus maze and open field tests. DSP-1053 modulates neurotransmitter levels in brain regions involved in mood regulation, including the prefrontal cortex, hippocampus, and raphe nuclei. The compound's ability to penetrate the blood-brain barrier and its favorable pharmacokinetic profile support its development as a potential antidepressant therapeutic.
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| Enzyme Assay |
In vitro receptor binding assays for DSP-1053 are performed using membrane preparations from cells expressing recombinant human SERT or 5-HT1A receptors. For SERT binding, [3H]-paroxetine or [3H]-citalopram is used as the radiolabeled ligand. Membranes are incubated with varying concentrations of DSP-1053 in assay buffer at room temperature for 1-2 hours. Bound and free radioligands are separated by rapid filtration through glass fiber filters. Filter-bound radioactivity is quantified by liquid scintillation counting. For 5-HT1A receptor binding, [3H]-8-OH-DPAT is used as the radioligand. Ki values are calculated using the Cheng-Prusoff equation. Non-specific binding is determined in the presence of excess unlabeled ligand.
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| Cell Assay |
In vitro cellular assays for DSP-1053 include serotonin uptake inhibition assays and 5-HT1A receptor functional assays. For uptake assays, human embryonic kidney (HEK-293) cells expressing human SERT are seeded in 96-well plates. Cells are incubated with [3H]-serotonin in the presence of serial dilutions of DSP-1053 for 5-10 minutes at 37degC. Uptake is terminated by washing with ice-cold buffer, and intracellular radioactivity is measured by scintillation counting. IC₅0 values for inhibition of serotonin uptake are calculated. For 5-HT1A receptor functional assays, cells expressing the receptor and a cAMP-responsive reporter are treated with DSP-1053 in the presence or absence of a full agonist (e.g., 8-OH-DPAT). cAMP levels are measured by ELISA or HTRF.
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| Animal Protocol |
In vivo animal studies for DSP-1053 are conducted in rodent models of depression and anxiety. Male C57BL/6 or Sprague-Dawley rats are administered DSP-1053 orally or intraperitoneally at doses of 1-30 mg/kg. The forced swim test is performed by placing animals in a cylinder of water for 6 minutes and measuring immobility time during the last 4 minutes. The tail suspension test measures immobility time in mice suspended by the tail for 6 minutes. The elevated plus maze assesses anxiety-like behavior by measuring time spent in open arms. Cognitive performance is evaluated using the novel object recognition test or Morris water maze. Brain serotonin levels and metabolite concentrations are measured by HPLC or LC-MS/MS. Pharmacokinetic parameters are determined from plasma and brain tissue samples.
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| ADME/Pharmacokinetics |
DSP-1053 (CAS#: 1176326-76-3) has molecular formula C2₆H32BrNO4 and molecular weight 502.44. The chemical name is 6-[2-(4-{[4-bromo-3-(2-methoxyethoxy)phenyl]methyl}piperidin-1-yl)ethyl]-3,4-dihydro-2H-1-benzopyran-4-one. The compound is a solid and should be stored at -20degC. DSP-1053 is a potent SERT inhibitor (Ki = 1.02 nM) with partial 5-HT1A receptor agonistic activity (Ki = 5.05 nM). The compound is soluble in DMSO. It is a research chemical for laboratory use only, not for human therapeutic applications.
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| Toxicity/Toxicokinetics |
Toxicological information for DSP-1053 is limited as the compound is a preclinical research chemical. Based on its mechanism as a serotonin modulator, potential adverse effects may include those typical of SSRIs and 5-HT1A agonists: gastrointestinal disturbances, headache, insomnia, sexual dysfunction, and serotonin syndrome at high doses or in combination with other serotonergic agents. The compound should be handled with standard laboratory precautions including the use of personal protective equipment and working in a well-ventilated area. Avoid inhalation, ingestion, and skin contact. The compound should be stored at -20degC and disposed of according to institutional guidelines for chemical waste.
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| References | |
| Additional Infomation |
DSP-1053 (CAS#: 1176326-76-3) is a novel benzylpiperidine derivative with a dual mechanism of action: potent serotonin transporter (SERT) inhibition (Ki = 1.02 nM) and partial 5-HT1A receptor agonism (Ki = 5.05 nM). This dual pharmacology is designed to provide rapid onset of antidepressant action and improved efficacy by simultaneously increasing synaptic serotonin levels and modulating autoreceptor-mediated feedback inhibition. The compound has shown antidepressant and cognitive-enhancing effects in preclinical models with a minimum effective dose of 3 mg/kg. DSP-1053 represents a potential next-generation antidepressant with a differentiated mechanism from conventional SSRIs. As of the current date, DSP-1053 remains a preclinical research compound and has not been approved for clinical use.
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| Molecular Formula |
C26H32BRNO4
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| Molecular Weight |
502.44
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| Exact Mass |
501.151
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| CAS # |
1176326-76-3
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| Related CAS # |
DSP-1053 benzenesulfonate;1176326-78-5
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| PubChem CID |
44182694
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.9
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
32
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| Complexity |
582
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1OC2=CC=C(CCN3CCC(CC4=CC=C(Br)C(OCCOC)=C4)CC3)C=C2C(=O)C1
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| InChi Key |
ZSVLGHSNQJYODD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H32BrNO4/c1-30-14-15-32-26-18-21(2-4-23(26)27)16-20-7-11-28(12-8-20)10-6-19-3-5-25-22(17-19)24(29)9-13-31-25/h2-5,17-18,20H,6-16H2,1H3
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| Chemical Name |
6-[2-[4-[[4-bromo-3-(2-methoxyethoxy)phenyl]methyl]piperidin-1-yl]ethyl]-2,3-dihydrochromen-4-one
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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 |
| 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 : ~200 mg/mL (~398.06 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9903 mL | 9.9514 mL | 19.9029 mL | |
| 5 mM | 0.3981 mL | 1.9903 mL | 3.9806 mL | |
| 10 mM | 0.1990 mL | 0.9951 mL | 1.9903 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.
Link: https://clinicaltrials.gov/ct2/show/NCT01774747
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