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RXFP2 agonist 6641

Chemical Structure : RXFP2 agonist 6641

CAS No.: 2971704-85-3

RXFP2 agonist 6641 (Compound 6641)

Catalog No.: PC-49427Not For Human Use, Lab Use Only.

RXFP2 agonist 6641 is a highly potent, selective and full allosteric agonist of relaxin/insulin-like family peptide receptor 2 (RXFP2) with EC50 of 0.38 uM, Emax=107% (hFXRP2).

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    Biological Activity

    RXFP2 agonist 6641 is a highly potent, selective and full allosteric agonist of relaxin/insulin-like family peptide receptor 2 (RXFP2) with EC50 of 0.38 uM, Emax=107% (hFXRP2).
    Compound 6641 is also activate the mouse RXFP2 receptor, does not activate either human or mouse RXFP1 receptors and RXFP3 or RXFP4 receptors.
    Compound 6641 is an allosteric agonist of RXFP2 that requires the RXFP2 transmembrane domain for activity.
    Compound 6641 (3-5 uM) induces gubernacular invagination in mouse embryos, induces osteoblast mineralization in human osteoblasts in vitro, specifically activates the mouse RXFP2 receptor in vivo.
    Compound 6641 treatment (10 mg/kg, PO) promotes bone formation in vivo.

    Physicochemical Properties

    M.Wt 787.377
    Formula C29H19F9IN3O5
    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

    (S)-8-(3,5-bis(trifluoromethyl)phenyl)-2-(2-(2-iodo-4-(trifluoromethoxy)phenoxy)acetyl)-1,3,4,12a-tetrahydrobenzo[e]pyrazino[1,2-a][1,4]diazepine-6,12(2H,11H)-dione

    References

    1. Esteban-Lopez M, et al. Commun Biol. 2022 Nov 4;5(1):1183.

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