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Compound 54149

Chemical Structure : Compound 54149

CAS No.: 2866254-56-8

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Compound 54149 (CaSR agonist 54149, (R)-85339)

Catalog No.: PC-21721Not For Human Use, Lab Use Only.

Compound 54149 is novel positive allosteric modulator (PAM) of calcium sensing receptor (CaSR) with EC50 of 41 nM.

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

    Biological Activity

    Compound 54149 is novel positive allosteric modulator (PAM) of calcium sensing receptor (CaSR) with EC50 of 41 nM.
    Compound 54149 stabilizes a distinct active-state CaSR dimer conformation.
    Compound 54149 suppresses PTH secretion better than the approved PAM drugs, inhibits PTH secretion dose-dependently (IC50=583 nM) in extracted parathyroid glands from wild-type (WT) C57/BL6 (B6) mice.
    Compound 54149 reduces serum PTH at lower doses with less hypocalcemia than cinacalcet and evocalcet.

    Physicochemical Properties

    M.Wt 326.41
    Formula C18H18N2O2S
    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

    (R)-1-(benzo[d][1,3]dioxol-4-yl)-N-(2-(benzo[d]isothiazol-3-yl)ethyl)ethan-1-amine

    References

    1. Liu F, et al. bioRxiv. 2023 Dec 27:2023.12.27.573448.
    2. Liu F, et al. Science. 2024 Sep 20;385(6715):eado1868.

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