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RXFP3/4 agonist 4

Chemical Structure : RXFP3/4 agonist 4

CAS No.: 2752378-80-4

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RXFP3/4 agonist 4

Catalog No.: PC-49433Not For Human Use, Lab Use Only.

RXFP3/4 agonist 4 is a potent, selective, nonpeptide dual RXFP3/4 agonist with EC50 of 82/2.0 nM in cellualr cAMP assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    RXFP3/4 agonist 4 is a potent, selective, nonpeptide dual RXFP3/4 agonist with EC50 of 82/2.0 nM in cellualr cAMP assays.
    RXFP3/4 agonist 4 also exhibits GTPγS binding EC50 values 119 nM for RXFP3 and 11 nM for RXFP4.
    RXFP3/4 agonist 4 also induces β-arrestin recruitment (EC50=4.9 uM relative to an EC50 of 83 nM for relaxin-3) in an RXFP3 overexpressing U2OS cell line.
    RXFP3/4 agonist 4 engages both G protein-mediated cAMP signaling and G protein-independent β-arrestin recruitment, a profile shared by relaxin-3.

    Physicochemical Properties

    M.Wt 383.880
    Formula C20H22ClN5O
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    (E)-N-(4-chlorophenethyl)-2-((7-ethyl-5-hydroxy-1H-indol-3-yl)methylene)hydrazine-1-carboximidamide

    References

    1. DeChristopher B, et al. Bioorg Med Chem Lett. 2019 Apr 15;29(8):991-994.

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