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

Ulotaront  (Synonyms: SEP-363856; SEP-856)

製品番号: HY-136109A
取扱説明書 Technical Support

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Ulotaront

Ulotaront 構造式

CAS 番号 : 1310426-33-5

容量 在庫状況
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製品説明

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)

体外実験

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.

体内実験

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.
臨床実験
分子量

183.27

分子式

C9H13NOS

CAS 番号
SMILES

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション
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  • 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.

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製品名:
Ulotaront
製品番号:
HY-136109A
数量:
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