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

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

Cat. No.: HY-136109 Purity: 99.57%
COA Handling Instructions

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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.

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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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 210 In-stock
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10 mg USD 310 In-stock
50 mg USD 800 In-stock
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Based on 5 publication(s) in Google Scholar

Other Forms of SEP-363856 hydrochloride:

SEP-363856 hydrochloride Related Antibodies

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[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) 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-363856 hydrochloride Related Antibodies
In Vivo

SEP-856 (0.3, 1 and 10 mg/kg, i.p.) hydrochloride 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) 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.

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.
Clinical Trial
Molecular Weight

219.73

Formula

C9H14ClNOS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

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
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 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

    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.
  • Protocol 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

    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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (455.10 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.57%

COA (254 KB) HNMR (251 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

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.

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SEP-363856 hydrochloride Related Classifications

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:

SEP-3638561310422-41-3SEP-856SEP363856SEP 363856SEP856SEP 8565-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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