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Purity: ≥98%
SEP-363856 HCL (also known as Ulotaront; SEP363856; SEP-856 HCL), is a novel and potent orally bioactive trace amine-associated receptor 1 (TAAR1) agonist with serotonin 1A (5-HT1A) agonist activity. Also a CNS active psychotropic agent with a Unique, Non-D 2 Receptor Mechanism of Action. It binds to 5-HT1A and trace amine-associated (TAAR) receptors instead of the dopamine-2 (D2) receptor, suggesting that it may be used to treat acute schizophrenia. Possibly used to treat additional neuropsychiatric conditions.
| Targets |
TAAR1 ( EC50 = 0.140 μM ); 5-HT1A Receptor ( EC50 = 2.3 μM ); 5-HT1B Receptor ( EC50 = 15.6 μM ); 5-HT1D Receptor ( EC50 = 0.262 μM ); 5-HT2A Receptor ( EC50 > 10 μM ); 5-HT2C Receptor ( EC50 = 30 μM ); 5-HT7 Receptor ( EC50 = 6.7 μM )
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| ln Vitro |
SEP-856 (10 μM) exhibits >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].
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| ln Vivo |
SEP-856 (0.3, 1 and 10 mg/kg, i.p.) has a behavioral signature resembling that of well-known antipsychotic medications and is CNS active[1].
SEP-856 (0.3, 1 and 10 mg/kg, orally once) substantially lowers hyperactivity brought on by PCP[1]. When SEP-856 is taken orally at doses of 1, 3, and 10 mg/kg, there is a dose-dependent reduction in REM sleep, an increase in REM sleep latency, and an increase in cumulative wake time [1]. |
| Animal Protocol |
Acute treatment with phencyclidine (PCP), which induces robust hyperactivity in rodents
0.3, 1 and 3 mg/kg Orally once. |
| References |
| Molecular Formula |
C9H14CLNOS
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|---|---|
| Molecular Weight |
219.7316
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| Exact Mass |
219.05
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| Elemental Analysis |
C, 49.20; H, 6.42; Cl, 16.13; N, 6.37; O, 7.28; S, 14.59
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| CAS # |
1310422-41-3
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| Related CAS # |
SEP-363856; 1310426-33-5; (Rac)-SEP-363856; 1310426-29-9; 2375116-24-6 (besylate); 2375116-27-9 (mesylate)
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| Appearance |
Solid powder
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| SMILES |
CNC[C@H]1C2=C(CCO1)C=CS2.Cl
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| InChi Key |
JRDQGVVFSHRVTL-QRPNPIFTSA-N
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| InChi Code |
InChI=1S/C9H13NOS.ClH/c1-10-6-8-9-7(2-4-11-8)3-5-12-9;/h3,5,8,10H,2,4,6H2,1H3;1H/t8-;/m0./s1
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| Chemical Name |
1-[(7S)-5,7-dihydro-4H-thieno[2,3-c]pyran-7-yl]-N-methylmethanamine;hydrochloride
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| Synonyms |
Ulotaront; Ulotaront HCl; Ulotaront hydrochloride; SEP 856; SEP-856; SEP856; SEP-363856; SEP 363856; SEP363856;
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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) |
H2O: ~100 mg/mL (~455.1 mM)
DMSO: ~62.5 mg/mL (~284.4 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (28.44 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 62.5 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: ≥ 6.25 mg/mL (28.44 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 62.5 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: ≥ 6.25 mg/mL (28.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (455.10 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.5510 mL | 22.7552 mL | 45.5104 mL | |
| 5 mM | 0.9102 mL | 4.5510 mL | 9.1021 mL | |
| 10 mM | 0.4551 mL | 2.2755 mL | 4.5510 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 |
| NCT04865835 | Completed | Drug: placebo Drug: SEP-363856 Drug: metformin |
Schizophrenia | Sumitomo Pharma America, Inc. | May 12, 2021 | Phase 1 |
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