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

Brilaroxazine  (Synonyms: RP5063)

Cat. No.: HY-109112 Purity: 98.29%
COA Handling Instructions

Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.

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

Brilaroxazine Chemical Structure

Brilaroxazine Chemical Structure

CAS No. : 1239729-06-6

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Description

Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors[1]. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo[2].

IC50 & Target[1][2]

5-HT1A Receptor

1.5 nM (Ki)

5-HT2A Receptor

2.5 nM (Ki)

5-HT2B Receptor

0.19 nM (Ki)

5-HT7 Receptor

2.7 nM (Ki)

D2 Receptor

 

D3 Receptor

 

D4 Receptor

 

In Vivo

Brilaroxazine (oral gavage; 10 mg/kg; twice daily; 28 days) limits the functional and structural effects of pulmonary arterial hypertension (PAH), with significant improvements in pulmonary hemodynamics, right ventricular (RV) hypertrophy, SO2, and pulmonary blood vessel structural changes[1].

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

Animal Model: SD-rats[2]
Dosage: 10 mg/kg
Administration: Oral gavage; twice daily; 28 days
Result: Had the efficacy in PAH, and mitigated the functional and structural effects of MCT-induced PAH.
Clinical Trial
Molecular Weight

450.36

Appearance

Solid

Formula

C22H25Cl2N3O3
CAS No.
SMILES

O=C1NC2=CC(OCCCCN3CCN(C(C=CC=C4Cl)=C4Cl)CC3)=CC=C2OC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (222.04 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2204 mL 11.1022 mL 22.2045 mL
5 mM 0.4441 mL 2.2204 mL 4.4409 mL
10 mM 0.2220 mL 1.1102 mL 2.2204 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: ≥ 2.5 mg/mL (5.55 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

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

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Keywords:

Brilaroxazine1239729-06-6RP5063RP 5063RP-5063Dopamine Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorPulmonaryarterialhypertensionPAHdepressivedisorder,Tourettesyndrome,ADHD AlzheimerParkinsonautismcardiacInhibitorinhibitorinhibit

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