1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. SEP-363856 hydrochloride

SEP-363856 hydrochloride (Synonyms: SEP-856 hydrochloride)

Cat. No.: HY-136109 Purity: 99.78%
Handling Instructions

SEP-363856 hydrochloride(SEP-856 hydrochloride), an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 hydrochloride(SEP-856 hydrochloride) has the potential for the treatment of schizophrenia.

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

SEP-363856 hydrochloride Chemical Structure

SEP-363856 hydrochloride Chemical Structure

CAS No. : 1310422-41-3

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5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

SEP-363856 hydrochloride(SEP-856 hydrochloride), an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 hydrochloride(SEP-856 hydrochloride) has the potential for the treatment of schizophrenia[1].

IC50 & Target

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-856 (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].

In Vivo

SEP-856 (0.3, 1 and 10 mg/kg, i.p.) is CNS active and exhibits a behavioral signature similar to known antipsychotic drugs[1].
SEP-856 (0.3, 1 and 10 mg/kg, orally once) significantly reduces PCP-induced hyperactivity[1].
Oral SEP-856 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].

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: 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.
Molecular Weight

219.73

Formula

C₉H₁₄ClNOS

CAS No.

1310422-41-3

SMILES

CNC[[email protected]]1C2=C(C=CS2)CCO1.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (284.44 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6.25 mg/mL (28.44 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

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

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SEP-363856 hydrochloride
Cat. No.:
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