2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Ulotaront

SEP-363856 (SEP-856), 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 (SEP-856) has the potential for the study of schizophrenia.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Ulotaront hydrochloride) that retains the same biological activity.

For research use only. We do not sell to patients.

Ulotaront

Ulotaront Chemical Structure

CAS No. : 1310426-33-5

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Ulotaront Related Antibodies

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Description

SEP-363856 (SEP-856), 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 (SEP-856) has the potential for the study of schizophrenia[1].

IC50 & Target[1]

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)

In Vitro

SEP-363856 (10 μM) 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.

Ulotaront Related Antibodies
In Vivo

SEP-363856 (0.3, 1 and 10 mg/kg, i.p.) is CNS active and exhibits a behavioral signature similar to known antipsychotic drugs[1].
SEP-363856 (0.3, 1 and 10 mg/kg, orally once) significantly reduces PCP-induced hyperactivity[1].
Oral SEP-363856 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.

Animal Model: Acute treatment with phencyclidine (PCP), which induces robust hyperactivity in rodents[1].
Dosage: 0.3, 1 and 3 mg/kg.
Administration: Orally once.
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.
Animal Model: Male Sprague Dawley rats[1].
Dosage: 1, 2, and 5 mg/kg.
Administration: I.V. injection. (Pharmacokinetic Analysis).
Result: 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.
Clinical Trial
Molecular Weight

183.27

Formula

C9H13NOS
CAS No.
SMILES

CNC[C@H]1C2=C(C=CS2)CCO1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Ulotaront Related Classifications

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Help & FAQs
  • 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:

Ulotaront1310426-33-5SEP-363856 SEP-856SEP363856SEP 363856SEP856SEP 856SEP-8565-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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