RP-5063( RP5063 )

Catalog No. M10967 CAS No. 1239729-06-6

RP-5063 (Brilaroxazine) is a multimodal dopamine and serotonin modulator with partial agonist activity at DA D2, D3, D4, 5-HT1A, and 5-HT2ARs, and antagonist activity at 5-HT2B, 5-HT6 and 5-HT7Rs.

Purity : >98% (HPLC)

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Biological Information

Product Name

RP-5063
Note

Research use only, not for human use.
Brief Description

RP-5063 (Brilaroxazine) is a multimodal dopamine and serotonin modulator with partial agonist activity at DA D2, D3, D4, 5-HT1A, and 5-HT2ARs, and antagonist activity at 5-HT2B, 5-HT6 and 5-HT7Rs.
Description

RP-5063 (Brilaroxazine) is a multimodal dopamine and serotonin modulator with partial agonist activity at DA D2, D3, D4, 5-HT1A, and 5-HT2ARs, and antagonist activity at 5-HT2B, 5-HT6 and 5-HT7Rs; produces dose-dependent reductions in pulmonary blood vessel wall thickness and proportion of muscular vessels, blocks MCT-induced increases in the plasma cytokines TNFα, IL-1β, and IL-6 in vivo; prevents Sugen 5416-hypoxia-induced pulmonary arterial hypertension in rats; improves declarative memory and psychosis in mouse models of schizophrenia.Schizophrenia Phase 2 Clinical.
In Vitro

——
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. Animal Model:SD-rats 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.
Synonyms

RP5063
Pathway

GPCR/G Protein
Target

Dopamine Receptor
Recptor

Dopamine Receptor
Research Area

Neurological Disease
Indication

Schizophrenia

Chemical Information

CAS Number

1239729-06-6
Formula Weight

450.36
Molecular Formula

C22H25Cl2N3O3
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 100 mg/mL (222.04 mM)
SMILES

C1CN(CCN1CCCCOC2=CC3=C(C=C2)OCC(=O)N3)C4=C(C(=CC=C4)Cl)Cl
Chemical Name

6-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-2H-benzo[b][1,4]oxazin-3(4H)-one

Shipping & Storage Information

Storage

(-20℃)
Shipping

With Ice Pack
Stability

≥ 2 years

Reference

1. Bhat L, et al. Eur J Pharmacol. 2017 Sep 5;810:83-91. 2. Rajagopal L, et al. Behav Brain Res. 2017 Aug 14;332:180-199. 3. Bhat L, et al. Eur J Pharmacol. 2017 Sep 5;810:92-99.

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