1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
    Dopamine Receptor
    Adrenergic Receptor
  3. Brexpiprazole

Brexpiprazole (Synonyms: OPC-34712)

Cat. No.: HY-15780 Purity: 99.64%
Handling Instructions

Brexpiprazole (OPC-34712), an atypical orally active antipsychotic drug, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).

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

Brexpiprazole Chemical Structure

Brexpiprazole Chemical Structure

CAS No. : 913611-97-9

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Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 61 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 77 In-stock
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50 mg USD 110 In-stock
Estimated Time of Arrival: December 31
100 mg USD 132 In-stock
Estimated Time of Arrival: December 31
200 mg USD 198 In-stock
Estimated Time of Arrival: December 31
500 mg USD 385 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

Brexpiprazole (OPC-34712), an atypical orally active antipsychotic drug, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[1][2].

IC50 & Target

5-HT1A Receptor

0.12 nM (Ki)

5-HT2A Receptor

0.47 nM (Ki)

D2L Receptor

0.3 nM (Ki)

human noradrenergic α1B

0.17 nM (Ki)

human noradrenergic α2C

0.59 nM (Ki)

In Vitro

Brexpiprazole (0-1.0 μM, 4 days) potentiates NGF-induced neurite outgrowth in a dose-dependent manner in PC12 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Brexpiprazole (0-0.1 mg/kg; p.o.; once) improves social recognition deficits in mice[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6NCrSlc mice, Dizocilpine (0.1 mg/kg) (HY-15084B) induced social recognition deficits[2]
Dosage: 0.01, 0.03 and 0.1 mg/kg
Administration: Oral administration, once
Result: Significantly ameliorated Dizocilpine-induced social recognition deficits, without sedation or a reduction of exploratory behavior.
Clinical Trial
Molecular Weight

433.57

Formula

C25H27N3O2S

CAS No.
SMILES

O=C1NC2=C(C=CC(OCCCCN3CCN(C4=C(C=CS5)C5=CC=C4)CC3)=C2)C=C1

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 : 25 mg/mL (57.66 mM; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3064 mL 11.5322 mL 23.0643 mL
5 mM 0.4613 mL 2.3064 mL 4.6129 mL
10 mM 0.2306 mL 1.1532 mL 2.3064 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.77 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.64%

References
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Product Name:
Brexpiprazole
Cat. No.:
HY-15780
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