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RP-5063

CAS No. 1239729-06-6

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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