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RLX-33

CAS No. 2784577-71-3

RLX-33( —— )

Catalog No. M35682 CAS No. 2784577-71-3

RLX-33 is a potent and selective antagonist of relaxin family peptide 3 (RXFP3) that crosses the blood-brain barrier and also blocks relaxin 3-induced ERK1/2 phosphorylation.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    RLX-33
  • Note
    Research use only, not for human use.
  • Brief Description
    RLX-33 is a potent and selective antagonist of relaxin family peptide 3 (RXFP3) that crosses the blood-brain barrier and also blocks relaxin 3-induced ERK1/2 phosphorylation.
  • Description
    RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome.
  • In Vitro
    ——
  • In Vivo
    RLX-33 (10 mg/kg; IP, single dosage) attenuates the RXFP3-selective agonist R3/I5-induced increase in feeding in male Wistar rats.RLX-33 (10 mg/kg; IP, single dosage) exhibits a good brain penetration and highly protein-bound in rats plasma. Pharmacokinetic Parameters of RLX-33 in male Wistar rats (IP, 10 mg/kg).Animal Model:Male Wistar rats (intracerebroventricular administration of R3/I5 stimulated food intake Dosage:10 mg/kg Administration:IP, single dosage Result:Attenuated the R3/I5-induced increase in food intake.Animal Model:Male Wistar rats Dosage:10 mg/kg Administration:IP, single dosage (Pharmacokinetic Analysis)Result:Exhibited a good brain penetration and highly protein-bound, with protein binding of 99.8% in rat plasma.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    RXFP receptor | ERK
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2784577-71-3
  • Formula Weight
    462.89
  • Molecular Formula
    C24H19ClN4O4
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 125 mg/mL (270.04 mM; Ultrasonic )
  • SMILES
    N(C(=O)C1CN(CC2=CC=CO2)C(=O)C1)C3=CC=C(C4=NC(=NO4)C5=CC=C(Cl)C=C5)C=C3
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. https://pubmed.ncbi.nlm.nih.gov/35594150/?
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