Ulotaront hydrochloride
Based on 11 publication(s) in Google Scholar
SEP-363856 (SEP-856) hydrochloride, an orally active TAAR1 and 5-HT1A agonist and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 hydrochloride has the potential for the study of schizophrenia.
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- Pureté: 99.89%
- CAS No.: 1310422-41-3
- Formule: C9H14ClNOS
- Masse moléculaire:219.73
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Ulotaront hydrochloride
More- Nature. 2024 Jun;630(8015):237-246. [Abstract]
- Nature. 2023 Dec;624(7992):672-681. [Abstract]
- Cell. 2023 Nov 22;186(24):5347-5362.e24. [Abstract]
- Adv Sci (Weinh). 2025 Oct 24:e02079. [Abstract]
- J Med Chem. 2025 Apr 10;68(7):7082-7105. [Abstract]
- Front Pharmacol. 2023 Apr 21:14:1161964. [Abstract]
- Drug Dev Res. 2024 Jun;85(4):e22225. [Abstract]
- World J Biol Psychiatry. 2024 Nov 29:1-18. [Abstract]
- Mol Pharmacol. 2025 Jul 28;107(9):100064. [Abstract]
- Synapse. 2025 Mar;79(2):e70011. [Abstract]
- patent. US20260034119A1.
Voir tous les produits spécifiques à Isoform 5-HT Receptor
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Activité biologique
|
5-HT1A Receptor |
TAAR1 0.140 μM (EC50) |
5-HT1A Receptor 2.3 μM (EC50) |
5-HT1B Receptor 15.6 μM (EC50) |
5-HT1D Receptor 0.262 μM (EC50) |
5-HT2A Receptor >10 μM (EC50) |
5-HT2C Receptor 30 μM (EC50) |
5-HT7 Receptor 6.7 μM (EC50) |
SEP-856 (10 μM) hydrochloride shows >50% inhibition of specific binding at α2A, α2B, D2, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SEP-856 (0.3, 1 and 10 mg/kg, orally once) hydrochloride significantly reduces PCP-induced hyperactivity[1].
Oral SEP-856 hydrochloride administration (1, 3 and 10 mg/kg) produces a dosedependent decrease in REM sleep, increase in latency to REM sleep and increase in cumulative wake (W) time[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute treatment with phencyclidine (PCP), which induces robust hyperactivity in rodents[1].
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Dosage:0.3, 1 and 3 mg/kg.
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Administration:Orally once.
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Result:Resulted in a dose-dependent inhibition of PCP-induced hyperactivity responses in C57Bl/6J mice (1-way ANOVA F (5, 59) = 18.96, p < 0.0001; Tukey’s post-hoc test, p < 0.05) with a 50% effective dose (ED50) of approximately 0.3 mg/kg.
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Animal Model:Male Sprague Dawley rats[1].
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Dosage:1, 2, and 5 mg/kg.
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Administration:I.V. injection. (Pharmacokinetic Analysis).
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Result:Rapidly absorbed with maximum plasma and brain concentrations reached within 0.25 to 0.5 hours in mice and rats and maximum plasma concentrations reached within 6 ± 2.83 hours in monkeys.
Penetrated mouse and rat brains after oral administration (10 mg/kg), with average brain-to-plasma AUC ratios of ~3 respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1310422-41-3
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Appearance Solid
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Masse moléculaire 219.73
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Formule C9H14ClNOS
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Color White to off-white
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SMILES
CNC[C@H]1C2=C(C=CS2)CCO1.Cl
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Synonyms
SEP-363856 hydrochloride; SEP-856 hydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (11)
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Journal Impact Factor
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Most Recent
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Nature
2024 Jun;630(8015):237-246. PMID: 38720072 -
Nature
2023 Dec;624(7992):672-681. PMID: 37935376 -
Cell
2023 Nov 22;186(24):5347-5362.e24. PMID: 37963465 -
Adv Sci (Weinh)
Cortico-Striatal-Midbrain Circuit Dysregulation Underlying MK-801 Induced Impulsivity and the Ameliorative Effects of SEP. [Abstract]2025 Oct 24:e02079. PMID: 41133933 -
J Med Chem
Rational Design of the First Dual Agonist at Trace Amine-Associated Receptor 1 and 5-HT2C Receptors Based on Binding Pocket Similarity for the Treatment of Schizophrenia and Alzheimer's Disease-Related Psychosis. [Abstract]2025 Apr 10;68(7):7082-7105. PMID: 40159850 -
Front Pharmacol
Biological evaluation and in silico studies of novel compounds as potent TAAR1 agonists that could be used in schizophrenia treatment. [Abstract]2023 Apr 21:14:1161964. PMID: 37153799 -
Drug Dev Res
SEP-363856 exerts neuroprotection through the PI3K/AKT/GSK-3β signaling pathway in a dual-hit neurodevelopmental model of schizophrenia-like mice. [Abstract]2024 Jun;85(4):e22225. PMID: 38879781 -
World J Biol Psychiatry
SEP-363856 attenuates CUMS-induced depression-like behaviours and reverses hippocampal neuronal injuries. [Abstract]2024 Nov 29:1-18. PMID: 39610275 -
Mol Pharmacol
Trace amine-associated receptor 1 agonists differentially regulate dopamine transporter function. [Abstract]2025 Jul 28;107(9):100064. PMID: 40840012 -
Synapse
Cellular-Resolution and Bulk-Fluorescence Recordings of Calcium Activity Yield Reciprocal Readouts of In Vivo Drug Efficacy. [Abstract]2025 Mar;79(2):e70011. PMID: 40013455 -
Solvant et solubilité
H2O : 100 mg/mL (455.10 mM; Need ultrasonic)
DMSO : 62.5 mg/mL (284.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 6.25 mg/mL (28.44 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 6.25 mg/mL (28.44 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (455.10 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 4.5510 mL | 22.7552 mL | 45.5104 mL | 113.7760 mL |
| 5 mM | 0.9102 mL | 4.5510 mL | 9.1021 mL | 22.7552 mL | |
| 10 mM | 0.4551 mL | 2.2755 mL | 4.5510 mL | 11.3776 mL | |
| 15 mM | 0.3034 mL | 1.5170 mL | 3.0340 mL | 7.5851 mL | |
| 20 mM | 0.2276 mL | 1.1378 mL | 2.2755 mL | 5.6888 mL | |
| 25 mM | 0.1820 mL | 0.9102 mL | 1.8204 mL | 4.5510 mL | |
| 30 mM | 0.1517 mL | 0.7585 mL | 1.5170 mL | 3.7925 mL | |
| 40 mM | 0.1138 mL | 0.5689 mL | 1.1378 mL | 2.8444 mL | |
| 50 mM | 0.0910 mL | 0.4551 mL | 0.9102 mL | 2.2755 mL | |
| 60 mM | 0.0759 mL | 0.3793 mL | 0.7585 mL | 1.8963 mL | |
| 80 mM | 0.0569 mL | 0.2844 mL | 0.5689 mL | 1.4222 mL | |
| 100 mM | 0.0455 mL | 0.2276 mL | 0.4551 mL | 1.1378 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.